pharm one liners
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Question Answer
Time it takes for amount of drug to fall to half of its value; thisis a constant in first order kinetics (majority of drugs)
Half-life (T1/2)
Relates the amount of drug in the body to the plasmaconcentration
Volume of distribution (VD)
Plasma concentration of a drug at a given time Cp
The ratio of the rate of elimination of a drug to its plasma
concentration Clearance (CL)The elimination of drug that occurs before it reaches thesystemic circulation
First pass effect
The fraction of administered dose of a drug that reachessystemic circulation
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination Steady state
This step of metabolism makes a drug more hydrophilic andhence augments elimination
Phase I
Different steps of Phase I Oxidation, reduction, hydrolysis
Inducers of Cytochrome P450 (CYP450) Barbiturates, phenytoin, carbamazepine, andrifampin
Inhibitors of CYP450Cimetidine, ketoconazole, erythromycin,isoniazid and grapefruit
Products of Phase II conjugationGlucuronate, acetic acid, and glutathionesulfate
Type of kinetics when a constant percentage of substrate ismetabolized per unit time
First order kinetics
Drug elimination with a constant amount metabolizedregardless of drug concentration
Zero order kinetics
Target plasma concentration times (volume of distributiondivided by bioavailability)
Loading dose (Cp*(Vd/F))
Concentration in the plasma times (clearance divided bybioavailability)
Maintenance dose (Cp*(CL/F))
Strength of interaction between drug and its receptor Affinity
Selectivity of a drug for its receptor Specificity
Amount of drug necessary to elicit a biologic effect; refers tothe drug's strength
Potency
Maximum response achieveable from a drug Efficacy
Ability of a drug to produce 100% of the maximum responseregardless of the potency Full agonist
Ability to produce less than 100% of the response Partial agonist
Ability to bind reversibly to the same site as the drug andwithout activating the effector system
Competitive antagonist
Class of drugs with ability to decrease the maximal response toan agonist
Noncompetitive antagonist
A hormone whose mechanism of action (MOA) utilizesintracellular receptors
Thyroid and steroid hormones
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A hormone whose MOA utilizes transmembrane receptors Insulin
Class of drugs whose MOA utilizes ligand gated ion channels Benzodiazepines and calcium channel blockers
Median effective dose required for an effect in 50% of thepopulation
ED50
Median toxic dose required for a toxic effect in 50% of thepopulation
TD50
Dose which is lethal to 50% of the population LD50
Window between therapeutic effect and toxic effect Therapeutic indexTerm for a high margin of safety High therapeutic index
Term for a narrow margin of safety Low therapeutic index
Antidote used for lead poisoning Dimercaprol, EDTA
Antidote used for cyanide poisoning Nitrites
Antidote used for anticholinergic poisoning Physostigmine
Antidote used for organophosphate/anticholinesterasepoisoning
Atropine, pralidoxime (2-PAM)
Antidote used for iron salt toxicity Deferoxamine
Antidote used for acetaminophen (APAP) toxicity N-acetylcysteine (Mucomyst)Antidote for arsenic, mercury, lead, and gold poisoning Dimercaprol
Antidote used in poisonings: copper (Wilson's disease), lead,mercury, and arsenic
Penicillamine
Antidote used for heparin overdose Protamine
Antidote used for warfarin toxicity Vitamin K and Fresh frozen plasma (FFP)
Antidote for tissue plasminogen activator (t-PA), streptokinase Aminocaproic acid
Antidote used for methanol and ethylene glycol Ethanol or fomepizole
Antidote used for opioid toxicity Naloxone (IV), naltrexone (PO)
Antidote used for benzodiazepine toxicity Flumazenil
Antidote used for tricyclic antidepressants (TCA) Sodium bicarbonate
Antidote used for carbon monoxide poisoning 100% O2 and hyperbaric O2
Antidote used for digitalis toxicityDigibind (also need to d/c digoxin, normalizeK+, and lidocaine if pt. Is arrhythmic)
Antidote used for beta agonist toxicity (eg. Metaproterenol) Esmolol
Antidote for methotrexate toxicity Leucovorin
Antidote for beta-blockers and hypoglycemia Glucagon
Antidote useful for some drug induced Torsade de pointes Magnesium sulfateAntidote for hyperkalemia sodium polystyrene sulfonate (Kayexalate)
Antidote for salicylate intoxication Alkalinize urine, dialysis
Constant proportion of cell population killed rather than aconstant number
Log-kill hypothesis
Treatment with cancer chemotherapy at high doses every 3-4weeks, too toxic to be used continuously
Pulse therapy
Toxic effect of anticancer drug can be lessened by rescueagents
Rescue therapy
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Drug used concurrently with toxic anticancer agents to reducerenal precipitation of urates
Allopurinol
Pyrimidine analog that causes "Thymine-less death"" givenwith leucovorin rescue"
5-flouracil (5-FU)
Drug used in cancer therapy causes Cushing-like symptoms Prednisone
Side effect of Mitomycin SEVERE myelosuppression
MOA of cisplatin Alkylating agent
Common toxicities of cisplatin Nephro and ototoxicityAnalog of hypoxanthine, needs HGPRTase for activation 6-mercaptopurine (6-MP)
Interaction with this drug requires dose reduction of 6-MP Allopurinol
May protect against doxorubicin toxicity by scavenging freeradicals
Dexrazoxane
Blows DNA (breaks DNA strands), limiting SE is pulmonaryfibrosis
Bleomycin
Bleomycin+vinblastine+etoposide+cisplatin produce almost a100% response when all agents are used for this neoplasm
Testicular cancer
ABVD regimen used for HD, but appears less likely to causesterility and secondary malignancies than MOPP Adriamycin (doxorubicin) +bleomycin,vinblastine +dacarbazine
Regimen used for non-Hodgkin's lymphomaCHOP (cyclophosphamide, doxorubicin,vincristine, and prednisone) plus rituximab
Regimen used for breast cancerCMF (cyclophosphamide, methotrexate, andfluorouracil) and tamoxifen if ER+
Alkylating agent, vesicant that causes tissue damage withextravasation
Mechlorethamine
Anticancer drug also used in RA, produces acrolein in urinethat leads to hemorrhagic cystitis
Cyclophosphamide
Prevention of cyclophosphamide induced hemorrhagic cystitis Hydration and mercaptoethanesulfonate(MESNA)
Microtubule inhibitor that causes peripheral neuropathy, footdrop (eg. ataxia), and "pins and needles"" sensation"
Vincristine
Interact with microtubules (but unlike vinca which preventdisassembly of tubules), it stabilizes tubulin and cells remainfrozen in metaphase
Paclitaxel (taxol)
Toxicities include nephrotoxicity and ototoxicity, leading to asevere interaction with aminoglycosides
Cisplatin
Agent similar to cisplatin, less nephrotoxic, but greater
myelosuppressionCarboplatin
Converts asparagine to aspartate and ammonia, denies cancercells of essential AA (asparagine)
L-asparaginase
Used for hairy cell leukemia; it stimulates NK cells Interferon alpha
Anti-androgen used for prostate cancer Flutamide (Eulexin)
Anti-estrogen used for estrogen receptor + breast cancer Tamoxifen
Aromatase inhibitor used in breast cancer Letrozole, anastrozole
Newer estrogen receptor antagonist used in advanced breastcancer
Toremifene (Fareston)
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Some cell cycle specific anti-cancer drugsBleomycin, vinca alkaloids, antimetabolites(eg., 5-FU, 6-MP, methotrexate, etoposide)
Some cell cycle non-specific drugsAlkylating agents (eg., mechlorethamine,cyclophosphamide), antibiotics (doxorubicin,daunorubicin), cisplatin, nitrosourea
Anti-emetics used in association with anti-cancer drugs thatare 5-HT3 (serotonin receptor subtype ) antagonists
Odansetron, granisetron
Nitrosoureas with high lipophilicity, used for brain tumors Carmustine (BCNU) and lomustine (CCNU)
Produces disulfiram-like reaction with ethanol Procarbazine
Somatostatin (SRIF) analog used for acromegaly, carcinoid,glucagonoma and other GH producing pituitary tumors
Octreotide
Somatotropin (GH) analog used in GH deficiency (dwarfism) Somatrem
GHRH analog used as diagnostic agent Sermorelin
GnRH agonist used for infertility or different types of CAdepending on pulsatile or steady usage respectively
Leuprolide
GnRH antagonist with more immediate effects, used forinfertility
Ganirelix
Dopamine (DA) agonist (for Parkinson's disease), used also forhyperprolactinemia
Bromocriptine
Hormone inhibiting prolactin release Dopamine
ACTH analog used for diagnosis of patients with corticosteroidabnormality
Cosyntropin
Synthetic analog of ADH hormone used for diabetes insipidusand nocturnal enuresis
Desmopressin (DDAVP)
SE of OCs Increased thromboembolic events
Most widely used thyroid drugs such as Synthroid andLevoxyl contain
L-thyroxine (T4)
T3 compound less widely used Cytomel
Anti-thyroid drugsThioamides, iodides, radioactive iodine, andipodate
Thioamide agents used in hyperthyroidism Methimazole and propylthiouracil (PTU)
Thioamide less likely to cross placenta, inhibits peripheralconversion of T4 to T3 in high doses, and should be used withextreme caution in pregnancy
PTU
PTU (propylthiouracil) MOAInhibits thyroid hormone synthesis by blockingiodination of the tyrosine residues of
thyroglobulinCan be effective for short term therapy of thyroid storm, butafter several weeks of therapy causes an exacerbation ofhyperthyroidism
Iodide salts
Dose may need to be increased during pregnancy or with Ocsdue to increased TBG in plasma
Thyroxine
Permanently cures thyrotoxicosis, patients will need thyroidreplacement therapy thereafter. Contraindicated in pregnancy
Radioactive iodine
Radio contrast media that inhibits the conversion of T4 to T3 Ipodate
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Block cardiac adverse effects of thyrotoxicosis such astachycardia, inhibits the conversion of T4 to T3
Beta-blockers such as propranolol
Vitamins containing iron should NOT be taken simultaneouslywith levothyroxine because
Iron deiodinates thyroxine
Thyroxine dose may need to be increased in hypothyroidpatient during pregnancy because
Estogens increase maternal TBG
3 zones of adrenal cortex and their productsGlomerulosa (mineralocorticoids), fasciculata(glucocorticoid=GC), and reticularis (adrenal
androgens)Pneumonic for 3 zones of adrenal cortex GFR
Used for Addison's disease, Congenital Adrenal Hyperplasia(CAH), inflammation, allergies, and asthma (as a localinhalation)
Glucocorticoids
Short acting glucocorticoidsCortisone and hydrocortisone (equivalent tocortisol)
Intermediate acting glucocorticoidsPrednisone, methylprednisolone, prednisolone,and triamcinolone
Long acting glucocorticoids Betamethasone and dexamethasoneMineralocorticoids Fludrocortisone and deoxycorticosterone
Some side effects of corticosteroidsOsteopenia, impaired wound healing, inc. riskof infection, inc. appetite, HTN, edema, PUD,euphoria, psychosis, stria, thinning of skin
Period of time of therapy after which GC therapy will need tobe tapered
5-7 days
Used for Cushing's syndrome (increased corticosteroid) Dexamethasone suppression test
Inhibits conversion of cholesterol to pregnenolone thereforeinhibiting corticosteroid synthesis
Aminoglutethimide
Antifungal agent used for inhibition of all gonadal and adrenalsteroids
Ketoconazole
Antiprogestin used as potent antagonist of GC receptor Mifepristone
Diuretic used to antagonize aldosterone receptors Spironolactone
Common SE of spironolactone Gynecomastia and hyperkalemia
Slightly increased risk of breast cancer, endometrial cancer,heart disease (questionable), has beneficial effects on bone loss
Estrogen
Antiestrogen drugs used for fertility and breast cancerrespectively
Clomiphene and tamoxifen
Common SE of tamoxifen and raloxifene Hot flashesSelective estrogen receptor modulator (SERM) used forprevention of osteoporosis and prophylaxis in women with riskfactors for breast cancer
Raloxifene
Non-steroidal estrogen agonist causes clear celladenocarcinoma of the vagina in daughters of women whoused it during pregnancy
Diethylstilbestrol (DES)
Estrogen mostly used in oral contraceptives (OC) Ethinyl estradiol and mestranol
Anti-progesterone used as abortifacient Mifepristone (RU-486)
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Constant low dose of estrogen and increasing dose of progestinfor 21 days (last 5 days are sugar pills or iron prep)
Combination oral contraceptives (OC)
Oral contraceptive available in a transdermal patch Ortho-Evra
Converted to more active form DHT by 5 alpha-reductase Testosterone
5 alpha-reductase inhibitor used for benign prostatichyperplasia (BPH) and male pattern baldness
Finasteride (Proscar and Propecia respectively)
Anabolic steroid that has potential for abuse Nandrolone, oxymetholone, and oxandrolone
Anti-androgen used for hirsutism in females Cyproterone acetateDrug is used with testosterone for male fertility Leuprolide
What do alpha cells in the pancreas produce? Glucagon
What do beta cells in the pancreas produce? Insulin
Where are beta cells found in the pancreas? Islets of Langerhans
What do delta cells in the pancreas produce? Somatostatin
Product of proinsulin cleavage used to assess insulin abuse C-peptide
Exogenous insulin contains Little C-peptide
Endogenous insulin contains Normal C-peptide
Very rapid acting insulin, having fastest onset and shortestduration of action
Lispro (Humalog), aspart, glulisine
Rapid acting, crystalline zinc insulin used to reverse acutehyperglycemia
Regular (Humulin R)
Long acting insulin Ultralente (humulin U)
Ultra long acting insulin, has over a day duration of action Glargine (Lantus), detemir
Major SE of insulin Hypoglycemia
Important in synthesis of glucose to glycogen in the liver GLUT 2
Important in muscle and adipose tissue for glucose transport
across muscles and TG storage by lipoprotein lipase activation GLUT 4Examples of alpha-glucosidase inhibitors (AGI) Acarbose, miglitol
MOA of AGI'sAct on intestine, delay digestion andabsorption of glucose formed from digestion ofstarch and disacchrides
SE of AGI'sFlatulence (do not use beano to tx), diarrhea,abdominal cramps
Alpha-glucosidase inhibitor associated with elevation of LFT's Acarbose
Amino acid derivative, active as an insulin secretagogue Nateglinide
MOA of nateglinide Insulin secretagogue - closes ATP-sensitiveK+ channel
Biguanide Metformin
Drugs available in combination with metformin Glyburide, glipizide, and rosiglitazone
MOA of metforminDecreases hepatic glucose production andintestinal glucose absorption; increase insulinsensitivity
Vascular effects of metformin Decreased micro and macro vascular disease
Most important potential SE of metformin Lactic acidosis
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Incidence of hyoglycemia with metformin
Meglitinide class of drugs Repaglinide
MOA of repaglinideInsulin release from pancreas; faster andshorter acting than sulfonylurea
First generation sulfonylurea Chlorpropamide, tolbutamide, tolazamide, etc.
Second generation sulfonylurea Glyburide, glipizide, glimepiride, etc.
MOA of both generationsInsulin release from pancreas by modifying K+
channelsCommon SE of sulfonylureas, repaglinide, and nateglinide Hypoglycemia
Sulfonylurea NOT recommended for elderly because of verylong half life
Chlorpropamide
ThiazolidinedionesPioglitazone, Rosiglitazone, Troglitazone(withdrawn/d from market)
Reason troglitazone was withdrawn from market Hepatic toxicity
MOA of thiazolindinedionesStimulate PPAR-gamma receptor to regulateCHO and lipid metabolism
SE of Thiazolindinediones Edema, mild anemia; interaction with drugsthat undergo CytP450 3A4 metabolism
Hyperglycemic agent that increases cAMP and results inglycogenolysis, gluconeogenesis, reverses hypoglycemia, alsoused to reverse severe beta-blocker overdose and smoothmuscle relaxation
Glucagon
Available bisphosphonatesAlendronate, etidronate, risedronate,pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates Inhibits osteoclast bone resorption
Names of three bisphosphonates available IV Pamidronate, zoledronate, ibandronate
Uses of bisphosphonates Osteoporosis, Paget's disease, and osteolyticbone lesions, and hypercalcemia frommalignancy
Major SE of bisphosphonates Chemical esophagitis
Bisphosphonates that cannot be used on continuous basisbecause it caused osteomalacia
Etidronate
Used for prevention of postmenopausal osteoporosis in women Estrogen (HRT-Hormone replacement therapy)
Increase bone density, also being tested for breast CAprophylaxis
Raloxifene (SERM-selective estrogen receptormodulator)
Used intranasally and decreases bone resorption Calcitonin (salmon prep)
Used especially in postmenopausal women, dosage should be1500 mg
Calcium
Vitamin given with calcium to ensure proper absorption Vitamin D
Disease caused by excess ergot alkaloids St. Anthony's Fire
Endogenous substances commonly interpreted as histamine,serotonin, prostaglandins, and vasoactive peptides
Autocoids
Syndrome of hypersecretion of gastric acid and pepsin usuallycaused by gastrinoma; it is associated with severe pepticulceration and diarrhea
Zollinger-Ellison Syndrome
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Drug that causes contraction of the uterus Oxytocin
Distribution of histamine receptors H1, H2, and H3Smooth muscle; stomach, heart, and mast cellsnerve endings, CNS respectively
Prototype antagonist of H1 and H2 receptors Diphenhydramine and cimetridine, respectively
1st generation antihistamine that is highly sedating Diphendydramine
1st generation antihistamine that is least sedating Chlorpheniramine or cyclizine
2nd generation antihistamines Fexofenadine, loratadine, and cetirizine
Generation of antihistamine that has the most CNS effects First generation due to being more lipid-soluble
Major indication for H1 receptor antagonist Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and isnot addictive
hydroxyzine (Atarax)
H1 antagonist used in motion sicknessDimenhydrinate, meclizine, and other 1stgeneration
Most common side effect of 1st generation antihistamines Sedation
Lethal arrhythmias resulting from concurrent therapy withazole fungals (metabolized by CYP 3A4) and theseantihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been
removed from the market)
H2 blocker that causes the most interactions with other drugs Cimetidine
Clinical use for H2 blockersAcid reflux disease, duodenal ulcer and pepticulcer disease
Receptors for serotonin (5HT-1) are locatedMostly in the brain, and they mediate synapticinhibition via increased K+ conductance
5HT-1d agonist used for migraine headaches Sumatriptan, naratriptan, and rizatriptan
Triptan available in parenteral and nasal formulation Sumatriptan
H1 blocker that is also a serotonin antagonist Cyproheptadine
Agents for reduction of postpartum bleeding Oxytocin, ergonovine and ergotamine
Agents used in treatment of carcinoid tumorKetanserin cyproheptadine, andphenoxybenzamine
5HT-3 antagonist used in chemotherapeutic induced emesisOndansetron, granisetron, dolasetron andalosetron
5HT-3 antagonist that has been associated with QRS and QTcprolongation and should not be used in patients with heartdisease
Dolasetron
DOC to treat chemo-induced nausea and vomiting Odansetron
Drug used in ergot alkaloids overdose, ischemia and gangrene NitroprussideReason ergot alkaloids are contraindicated in pregnancy Uterine contractions
SE of ergot alkaloids Hallucinations resembling psychosis
Ergot alkaloid used as an illicit drug LSD
Dopamine agonist used in hyperprolactinemia Bromocriptine
Peptide causing increased capillary permeability and edema Bradykinin and histamine
Mediator of tissue pain, edema, inactivated by ACE, and maybe a contributing factor to the development of angioedema
Bradykinin
Drug causing depletion of substance P (vasodilator) Capsaicin
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Prostaglandins that cause abortionsProstaglandin E1 (misoprostol) PGE2, andPGF2alpha
Difference between COX 1 and COX 2COX 1 is found throughoutthe body and COX2 is onlyin inflammatory tissue
Drug that selectively inhibits COX 2 Celecoxib and rofecoxib
Inhibitor of lipoxygenase Zileuton
Major SE of zileuton Liver toxicity
Inhibitor of leukotrienes (LTD4) receptors and used in asthma Zafirlukast and montelukastUsed in pediatrics to maintain patency of ductus arteriosis PGE1
Approved for use in severe pulmonary HTN PGI2 (epoprostenol)
Prostaglandin used in the treatment of impotence Alprostadil
Irreversible, nonselective COX inhibitor Aspirin
Class of drugs that reversibly inhibit COX NSAIDS
Primary endogenous substrate for Nitric Oxidase Synthase Arginine
MOA and effect of nitric oxideStimulates cGMP which leads to vascularsmooth muscle relaxation
Long acting beta 2 agonist used in asthma Salmeterol
Muscarinic antagonist used in asthma Ipratropium
MOA of cromolyn Mast cell stabilizer
Methylxanthine derivative used as a remedy for intermittentclaudication
Pentoxifylline
MOA of corticosteroids inhibit phospholipase A2
SE of long term (>5 days) corticosteroid therapy and remedyAdrenal suppression and weaning slowly,respectively
MOA of quinolones Inhibit DNA gyrase
MOA of penicillin Block cell wall synthesis by inhibitingpeptidoglycan cross-linkage
Drug used for MRSA Vancomycin
Vancomycin MOA Blocks peptidoglycan synthesis
Type of resistance found with vancomycin Point mutation
Meningitis prophylaxis in exposed patients Rifampin
Technique used to diagnose perianal itching, and the drug usedto treat it
Scotch tape technique and mebendazole
Two toxicities of aminoglycosides nephro and ototoxicity
DOC for Legionnaires' disease Erythromycin
MOA of sulfonamides Inhibit dihydropteroate synthase
Penicillins active against penicillinase secreting bacteria Methicillin, nafcillin, and dicloxacillin
Cheap wide spectrum antibiotic DOC for otitis media Amoxicillin
Class of antibiotics that have 10% cross sensitivity withpenicillins
Cephalosporins
PCN active against pseudomonas Carbenicillin, piperacillin and ticarcillin
Antibiotic causing red-man syndrome, and preventionVancomycin, infusion at a slow rate and
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antihistamines
Drug causes teeth discoloration Tetracycline
MOA of tetracyclineDecreases protein synthesis by inhibiting 30Sribosome
Drug that causes gray baby syndrome and aplastic anemia Chloramphenicol
Drug notorious for causing pseudomembranous colitis Clindamycin
DOC for tx of pseudomembranous colitis Metronidazole
Treatment of resistant pseudomembranous colitis ORAL vancomycinAnemia caused by trimethoprim Megaloblastic anemia
Reason fluoroquinolones are contraindicated in children andpregnancy
Cartilage damage
DOC for giardia, bacterial vaginosis, pseudomembranouscolitis, and trichomonas
Metronidazole
Treatment for TB patients (think RIPE)Rifampin, Isoniazid, Pyrazinamide, andEthambutol
Metronidazole SE if given with alcohol Disulfiram-like reaction
Common side effect of Rifampin Red urine discolorationMOA of nystatin Bind ergosterol in fungal cell membrane
Neurotoxicity with isoniazid (INH) prevented by Administration of Vit. B6 (pyridoxine)
Toxicity of amphotericin Nephrotoxicity
SE seen only in men with administration of ketoconazole Gynecomastia
Topical DOC in impetigo Topical mupirocin (Bactroban)
DOC for influenza A Amantadine
DOC for RSV Ribavirin
DOC for CMV retinitis Ganciclovir
SE for ganciclovir Neutro, leuko and thrombocytopenia
Anti-viral agents associated with Stephen Johnson syndrome Nevirapine, amprenavir
HIV antiviral class known to have severe drug interactions bycausing inhibition of metabolism
Protease inhibitors
Antivirals that are teratogens Delavirdine, efavirenz, and ribavirin
Antivirals associated with neutropeniaGanciclovir, zidovudine, saquinavir, andinterferon
HIV med used to reduce transmission during birth AZT (zidovudine)
Drug used for African sleeping sickness Suramin
Drug used in Chagas disease Nifurtimox
Cephalosporins able to cross the BBBCefuroxime (2nd) generation, Ceftazidime,Ceftriaxone
Cephalosporins NOT able to cross the BBB Cefixime (3rd) generation
Drug used for N. gonorrhea in females Ceftriaxone
Cephalosporin causes kernicterus in neonates Ceftriaxone or cefuroxime
SE of INH Peripheral neuritis and hepatitis
Aminoglycoside that is least ototoxic Streptomycin
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Drug used in exoerythrocytic cycle of malaria Primaquine
Oral antibiotic of choice for moderate inflammatory acne Minocycline
Drug of choice for leprosyDapsone, rifampin and clofaziminecombination
DOC for herpes and its MOAAcyclovir; incorporated into viral DNA andchain termination
Anti-microbials that cause hemolysis in G6PD-deficientpatients
Sulfonamides
MOA of erythromycinInhibition of protein synthesis at the 50ssubunit of ribosome
Anti-biotic frequently used for chronic UTI prophylaxis sulfamethoxazole/ trimethoprim
Lactam that can be used in PCN allergic patients Aztreonam
SE of imipenem Seizures
Anti-viral with a dose limiting toxicity of pancreatitis Didanosine
Common side effect of hypnotic agents Sedation
Occurs when sedative hypnotics are used chronically or at highdoses
Tolerance
The most common type of drug interaction of sedativehypnotics with other depressant medications
Additive CNS depression
Benzodiazepines used to promote sleep Temazpam, trizolam, flurazepam
Benzodiazepine used for anxiety Alprazolam
Non-benzodiazepine used as an anxiolytic Buspirone
Non-benzodiazepine used for sleep Zolpidem
Major effect of benzodiazepines on sleep at high doses REM is decreased
Neurologic SE of benzodiazepines Anterograde amnesia
Reason benzos are used cautiously in pregnancy Ability to cross the placentaMain route of metabolism for benzodiazepines Hepatic
Benzodiazepine that undergo extrahepatic conjugation (whichare useful in older or hepatically impaired)
Lorazepam, oxazepam, and temazepam
MOA for benzodiazepinesincrease the FREQUENCY of GABA-mediated chloride ion channel opening
Antidote to benzodiazepine overdose (antagonist that reversesthe CNS effects)
Flumazenil
Benzodiazepine with useful relaxant effects in skeletal musclespasticity of central origin
Diazepam
Benzodiazepine that has efficacy against absence seizures andin anxiety states, such as agoraphobia
Clonazepam
Benzodiazepines that are the most effective in the treatment ofpanic disorder
Alprazolam and Clonazepam
Benzodiazepine that is used for anesthesia Midazolam
DOC for status epilepticus Diazepam
Longer acting benzodiazepines used in the management ofwithdrawal states of alcohol and other drugs
Chlordiazepoxide and Diazepam
Agents having active metabolites, long half lives, and a high Diazepam, Flurazepam, chlordiazepoxide, and
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incidence of adverse effects clorazepate
Barbiturates
Barbiturates may precipitate this hematologic condition Acute intermittent porphyria
Barbiturates decrease the effectiveness of many other drugs viathis pharmacokinetics property
Liver enzyme INDUCTION
Barbiturates MOAIncrease the DURATION of GABA-mediatedchloride ion channels
Barbiturate used for the induction of anesthesia ThiopentalSite of action for zaleplon and zolpidem
Benzodiazepine receptor BZ1 (although do nothave a benzodiazepine ring structure)
Good hypnotic activity with less CNS SE than mostbenzodiazepines
Zolpidem, zaleplon
Agent that is a partial agonist for the 5-HT1A receptor Buspirone
Drug of choice for generalized anxiety disorder, NOT effectivein acute anxiety
Buspirone
Agent that is metabolized to acetaldehyde by alcoholdehydrogenase and microsomal ethanol-oxidizing system
(MEOS)
Ethanol
Agent with zero-order kinetics Ethanol
Rate limiting step of alcohol metabolism Aldehyde dehydrogenase
System that increases in activity with chronic ethanol exposureand may contribute to tolerance
MEOS
Enzyme that metabolizes acetaldehyde to acetate Aldehyde dehydrogenase
Agents that inhibit acetaldehyde dehydrogenaseDisulfiram, metronidazole, certainsulfonylureas and cephalosporins
Agent that inhibits alcohol dyhydrogenase and its clinical use
FOMEPIZOLE used to prevent formation
of toxic metabolites from methanol andethylene glycol ingestion
Agent used in the treatment of alcoholism, if alcohol isconsumed concurrently, acetaldehyde builds up and results innausea, headache, flushing, and hypotension
Disulfiram
The most common neurologic abnormality in chronicalcoholics
Peripheral neuropathy (also excessive alcoholuse is associated with HTN, anemia, and MI)
Agent that is teratogen and causes a fetal syndrome Ethanol
Agent that is the antidote for methanol overdose Ethanol, fomepizole
Drug that inhibits alcohol dehydrogenase and is used in
ethylene glycol exposure FomepizoleMost frequent route of metabolism Hepatic enzymes
Mechanisms of action for Phenytoin, Carbamazepine,Lamotrigine
Sodium channel blockade
MOA for benzodiazepines and barbiturates GABA-related targets
MOA for Ethosuximide Calcium channels
MOA for Valproic acid at high dosesAffect calcium, potassium, and sodiumchannels
Drugs of choice for generalized tonic-clonic and partial
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seizuresValproic acid and Phenytoin
DOC for febrile seizures Phenobarbital
Drugs of choice for absence seizures Ethosuximide and valproic acid
Drug of choice for myoclonic seizures Valproic acid
Drugs of choice for status epilepticusIV diazepam for short term (acute) treatment;phenytoin for prolonged therapy
Drugs that can be used for infantile spasms Corticosteroids
Anti-seizure drugs used also for bipolar affective disorder(BAD)
Valproic acid, carbamazepine, phenytoin andgabapentin
Anti-seizure drugs used also for Trigeminal neuralgia Carbamazepine
Anti-seizure drugs used also for pain of neuropathic orgin Gabapentin
Anti-seizure agent that exhibits non-linear metabolism, highlyprotein bound, causes fetal hydantoin syndrome, and stimulateshepatic metabolism
Phenytoin
SE of phenytoinGingival hyperplasia, nystagmus, diplopia andataxia
Anti-seizure agent that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofacialanomalies and spina bifida
Carbamazepine
Agent that inhibits hepatic metabolism, is hepatotoxic andteratogen that can cause neural tube defects andgastrointestinal distress
Valproic acid
Laboratory value required to be monitored for patients onvalproic acid
Serum ammonia and LFT's
SE for Lamotrigine Stevens-Johnson syndrome
SE for Felbamate Aplastic anemia and acute hepatic failure
Anti-seizure medication also used in the prevention ofmigraines
Valproic acid
Carbamazepine may cause Agranulocytosis
Anti-seizure drugs used as alternative drugs for moodstabilization
Carbamazepine, gabapentin, lamotrigine, andvalproic acid
MOA of general anestheticsMost are thought to act at GABA-A receptor -chloride channel
Inhaled anesthetic with a low blood/gas partition coefficient Nitrous oxide
Inversely related to potency of anestheticsMinimum alveolar anesthetic concentration
(MAC)Inhaled anesthetics metabolized by liver enzymes which has amajor role in the toxicity of these agents
Halothane and methoxyflurane
Most inhaled anesthetics SE Decrease arterial blood pressure
Inhaled anesthetics are myocardial depressants Enflurane and halothane
Inhaled anesthetic causes peripheral vasodilation Isoflurane
Inhaled anesthetic that may sensitize the myocardium toarrhythmogenic effects of catecholamines and has producedhepatitis
Halothane
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Inhaled anesthetic, less likely to lower blood pressure thanother agents, and has the smallest effect on respiration
Nitrous oxide
Fluoride released by metabolism of this inhaled anesthetic maycause renal insufficiency
Methoxyflurane
Prolonged exposure to this inhaled anesthetic may lead tomegaloblastic anemia
Nitrous oxide
Pungent inhaled anesthetic which leads to high incidence ofcoughing and vasospasm
Desflurane
DOC for malignant hyperthermia that may be caused by use ofhalogenated anesthetics
Dantrolene
IV barbiturate used as a pre-op anesthetic Thiopental
Benzodiazepine used adjunctively in anesthesia Midazolam
Benzodiazepine receptor antagonist, it accelerates recoveryfrom benzodiazepine overdose
Flumazenil
This produces "dissociative anesthesia"", is a cardiovascularstimulant which may increases intracranial pressure, andhallucinations occur during recovery"
Ketamine
Opioid associated with respiratory depression, but is used inhigh risk patients who may not survive full general anesthetia Fentanyl
State of analgesia and amnesia produced when fentanyl is usedwith droperidol and nitrous oxide
Neuroleptanesthesia
Produces both rapid anesthesia and recovery, has antiemeticactivity and commonly used for outpatient surgery, may causemarked hypotension
Propofol
MOA of local anesthetics (LA's) Block voltage-dependent sodium channels
This may enhance activity of local anesthetics Hyperkalemia
This may antagonize activity of local anesthetics Hypercalcemia
Almost all local anesthetics have this property and sometimesrequire the administration of vasoconstrictors (ex. Epinephrine)to prolong activity
Vasodilation
Local anesthetic with vasoconstrictive property, favored forhead, neck, and pharyngeal surgery
Cocaine
Longer acting local anesthetics which are less dependent onvasoconstrictors
Tetracaine and bupivacaine
These LA's have surface activity Cocaine and benzocaine
Most important toxic effects of most local anesthetics CNS toxicity
Commonly abused LA which has cardiovascular toxicityincluding severe hypertension with cerebral hemorrhage,cardiac arrhythmias, and myocardial infarction
Cocaine
LA causing methemoglobinemia Prilocaine
Structurally related to acetylcholine, used to produce muscleparalysis in order to facilitate surgery or artifical ventilation.Full doses lead to respiratory paralysis and require ventilation
Neuromuscular blocking drugs
These drugs strongly potentiate and prolong effect ofneuromuscular blockade (NMB)
Inhaled anesthetics, especially isoflurane,aminoglycosides, and antiarrhythmic
These prevent the action of Ach at the skeletal muscle endplate
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to produce a "surmountable blockade,"" effect is reversed bycholinesterase inhibitors (ex. neostigmine or pyridostigmine)"
Nondepolarizing type antagonists
Agent with long duration of action and is most likely to causehistamine release
Tubocurarine
Non-depolarizing skeletal muscle antagonist that has shortduration
Mivacurium
Skeletal muscle agent that can block muscarinic receptors Pancuronium
Skeletal muscle agent that undergoes Hofmann elimination(breaks down spontaneously) Atracurium
One depolarizing blocker that causes continuous depolarizationand results in muscle relaxation and paralysis, causes musclepain postoperatively and myoglobinuria may occur
Succinylcholine
During Phase I these agents worsen muscle paralysis bysuccinylcholine, but during phase II they reverse the blockadeproduced by succinylcholine
Cholinesterase inhibitors
Agents acting in the CNS or in the skeletal muscle, used toreduce abnormally elevated tone caused by neurologic ormuscle end plate disease
Spasmolytic drugs
Facilitates GABA presynaptic inhibition Diazepam
GABA agonist in the spinal cord Baclofen
Similar to clonidine and may cause hypotension Tizanidine
DOC for malignant hyperthermia by acting on thesacroplasmic reticulum or skeletal muscle
Dantrolene
Agent used for acute muscle spasm Cyclobenzaprine
Irreversible condition resulting from the use of antipsychotics,reserpine at high doses, and MPTP (by-product of illicitmeperidine analog)
Drug induced Parkinsonism
Agent used in drug therapy of Parkinson's instead ofDopamine which has low bioavailability and does not cross theBBB
L-dopa
This is combined with L-dopa, inhibits DOPA decarboxylase(active only peripherally) which allows lower effective dosesof L-dopa and allows for fewer SE's (GI distress, posturalhypotension, and dyskinesias)
Carbidopa
Clinical response that may fluctuate in tx of Parkinson's dx "On-off-phenomenon"" "
Anti-Parkinson's drug which increases intraocular pressure andis contraindicated in closed angle glaucoma
Levodopa
Ergot alkaloid that is a partial agonist at D2 receptors in thebrain, used for patients who are refractory or cannot toleratelevodopa, causes erythromelalgia
Bromocriptine
Non ergot agents used as first-line therapy in the initialmanagement of Parkinson's
Pramipexole and ropinirole
Enhances dopaminergic neurotransmission SE's include CNSexcitation, acute toxic psychosis and livedo reticularis
Amantadine
Inhibitor of MAO type B which metabolizes dopamine, usedadjunct to levodopa or as sole agent in newly diagnosedpatients
Selegiline
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Inhibitors of catechol-O-methyltransferase (COMT), used asadjuncts in Parkinson's dx and cause acute hepatic failure(monitor LFT's)
Entacapone and Tolcapone
Agent decreases the excitatory actions of cholinergic neurons.May improve tremor and rigidity but have LITTLE effect onbradykinesia. Atropine-like side effects
Benztropine
Agent effective in physiologic and essential tremor Propranolol
Agents used in Huntington's DiseaseTetrabenazine (amine depleting drug),Haloperidol (antipsychotic)
Agents used in Tourette's dx Haloperidol or pimozide
Chelating agent used in Wilson's disease Penicillamine
Extrapyramidal dysfunction is more common with theseagents, which block this subtype of dopamine receptor
Older antipsychotic agents, D2 receptors
MOA of neuroleptics Dopamine blockade
Side effects occuring in antipsychotics that block dopamineHyperprolactinemia, menorrhea, galactorrhea,confusion, mood changes, decreased sexualinterest, and weight gain
Antipsychotics that reduce positive symptoms only Older antipsychoticsNewer atypical antipsychotics that also improve some of thenegative symptoms and help acute agitation
Olanzapine, aripiprazole, and sertindole
Antipsychotic used in the treatment of psychiatric symptoms inpatients with dementia
Risperidone
Atypical antipsychotic causing high prolactin levels Risperidone
Newer atypical antipsychotic used for bipolar disorder, knownto cause weight gain, and adversely affect diabetes
Olanzapine
Agent more frequently associated with extrapyramidal sideeffects that can be treated with benzodiazepine,diphenhydramine or muscarinic blocker
Haloperidol
Drug used in neuroleptic malignant syndrome Dantrolene
Agents may exacerbate tardive dyskinesias (may beirreversible and there is no treatment)
Muscarinic blockers
Antipsychotic having the strongest autonomic effects Thioridazine
Antipsychotic having the weakest autonomic effects Haloperidol
Only phenothiazine not exerting antiemetic effects, can causevisual impairment due to retinal deposits, and high doses havebeen associated with ventricular arrhythmias
Thioridazine
Agent having no effect on D2 receptors, blocks D4, reservedfor resistant schizophrenia, and can cause fatal agranulocytosis
Clozapine
Anti-psychotic not shown to cause tardive dyskinesia Clozapine
Anti-psychotics available in depot preparation Fluphenazine and haloperidol
Reduced seizure thresholdLow-potency typical antipsychotics andclozapine
Orthostatic hypotension and QT prolongation Low potency phenothiazines and ziprasidone
Increased risk of developing cataracts Quetiapine
Major route of elimination for Lithium Kidneys
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Patients being treated with lithium, who are dehydrated, ortaking diuretics concurrently, could develop
Lithium toxicity
Drug increases the renal clearance hence decreases levels oflithium
Theophylline
Lithium is associated with this congenital defectCardiac anomalies and is contraindicated inpregnancy or lactation
DOC for bipolar affective disorder Lithium
Concern using lithium Low therapeutic indexSE of lithium
Tremor, sedation, ataxia, aphasia, thyroidenlargement, and reversible diabetes insipidus
Example of three antidepressants that are indicated forobsessive compulsive disorder
Clomipramine, fluoxetine and fluvoxamine
Neurotransmitters affected by the action of antidepressants Norepinephrine and serotonin
Usual time needed for full effect of antidepressant therapy 2 to 3 weeks
Population group especially sensitive to side effects ofantidepressants
Elderly patients
All antidepressants have roughly the same efficacy in treatingdepression, agents are chosen based on these criterion Side-effect profile and prior pt response
Well-tolerated and are first- line antidepressants SSRI's, bupropion, and venlafaxine
Most useful in patients with significant anxiety, phobicfeatures, hypochondriasis, and resistant depression
Monamine oxidase inhibitors
Condition will result from in combination of MAOI withtyramine containing foods (ex. wine, cheese, and pickledmeats)
Hypertensive crisis
MAOI should not be administered with SSRI's or potent TCA'sdue to development of this condition
Serotonin syndrome
Sedation is a common side effect of these drugs, they lowerseizure threshold, uses include BAD, acute panic attacks,phobias, enuresis, and chronic pain and their overdose can bedeadly
Tricyclic antidepressants (TCA)
Three C's associated with TCA toxicityComa, Convulsions, Cardiac problems(arrhythmias and wide QRS)
Agents having higher sedation and antimuscarinic effects thanother TCA's
Tertiary amines
TCA used in chronic pain, a hypnotic, and has markedantimuscarinic effects
Amitriptyline
TCA used in chronic pain, enuresis, and ADD ImipramineTCA with greatest sedation of this group, and markedantimuscarinic effects, used for sleep
Doxepin
TCA used in obsessive compulsive disorder (OCD), mostsignificant of TCA's for risk of seizure, weight gain, andneuropsychiatric signs and symptoms
Clomipramine
Secondary amines that have less sedation and more excitationeffect
Nortriptyline, Desipramine
Side effects seen with tricyclic antidepressantsMuscarinic blockade (dry mouth, constipation)weak alpha-1 block (orthostatic hypotension);
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weak hisamine block (sedation)
Antidepressant associated with neuroleptic malignantsyndrome
Amoxapine
Antidepressant associated with seizures and cardiotoxicity Maprotiline
Antidepressant having stimulant effects similar to SSRI's andcan increase blood pressure
Venlafaxine
Antidepressant inhibiting norepinephrine, serotonin, anddopamine reuptake
Venlafaxine
Antidepressant also used for sleep that causes priapism Trazodone
Antidepressant which is inhibitor of CYP450 enzymes andmay be associated with hepatic failure
Nefazodone
Heterocyclic antidepressants least likely to affect sexualperformance, used for management of nicotine withdrawal,SE's include dizziness, dry mouth, aggravation of psychosis,and seizures
Bupropion
Antidepressant with MOA as alpha 2 antagonist, has effects onboth 5-HT and NE, blocks histamine receptors, and is sedating
Mirtazapine
SE of mirtazapine Liver toxicity, increased serum cholesterolExcept for these agents all SSRI have significant inhibition ofCytP450 enzymes
Citalopram and its metabolite escitalopram
Side effects frequently seen with SSRIs CNS stimulation; GI upset
Antidepressants with no effect on BP, no sedation SSRIs
SSRI with long T1/2 and can be administered once weekly formaintenance, not acute tx
Fluoxetine
SSRI indicated for premenstrual dysphoric disorder Fluoxetine (Sarafem)
Some of SSRIs' therapeutic effects beside depression
Panic attacks, social phobias, bulimia nervosa,
and PMDD (premenstrual dysphoric disorder),OCD
SSRI less likely to cause a withdrawal syndrome Fluoxetine
Inhibit synaptic activity of primary afferents and spinal cordpain transmission neurons
Ascending pathways
Activation of these receptors close Ca2+ ion channels to inhibitneurotransmitter release
Presynaptic mu, delta, and kappa receptors
Activation of these receptors open K+ ion channels to causemembrane hyperpolarization
Postsynaptic Mu receptors
Tolerance to all effects of opioid agonists can develop except Miosis and constipation
All opioids except this agent (which has a muscarinic blockingaction) cause pupillary constriction
Meperidine
SE of these drugs include dependence, withdrawal syndrome,sedation, euphoria, respiratory depression nausea andvomiting, constipation, biliary spasm, increased ureteral andbladder tone, and reduction in uterine tone
Opioid Analgesics
Strong opioid agonistsMorphine, methadone, meperidine, andfentanyl
Opioids used in anesthesia Morphine and fentanyl
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Opioid used in the management of withdrawal states Methadone
Opioid available trans-dermally Fentanyl
Opioid that can be given PO, by epidural, and IV, which helpsto relieve the dyspnea of pulmonary edema
Morphine
Use of this opioid with MAOI can lead to hyperpyrexic coma,and with SSRI's can lead to serotonin syndrome
Meperidine
Moderate opioid agonists Codeine, hydrocodone, and oxycodone
Weak opioid agonist, poor analgesic, its overdose can causesevere toxicity including respiratory depression, circulatorycollapse, pulmonary edema, and seizures
Propoxyphene
Partial opioid agonist, considered a strong analgesic, has along duration of action and is resistant to naloxone reversal
Buprenorphine
Opioid antagonist that is given IV and had short DOA Naloxone
Opioid antagonist that is given orally in alcohol dependencyprograms
Naltrexone
These agents are used as antitussive Dextromethorphan, Codeine
These agents are used as antidiarrheal Diphenoxylate, Loperamide
Inhalant anesthetics NO, chloroform, and diethyl ether
Toxic to the liver, kidney, lungs, bone marrow, peripheralnerves, and cause brain damage in animals, sudden death hasoccurred following inhalation
Fluorocarbons and Industrial solvents
Cause dizziness, tachycardia, hypotension, and flushing Organic nitrites
Causes acne, premature closure of epiphyses, masculinizationin females, hepatic dysfunction, MI, and increases in libidoand aggression
Steroids
Readily detected markers that may assist in diagnosis of the
cause of a drug overdose include
Changes in heart rate, blood pressure,
respiration, body temperature, sweating, bowelsigns, and pupillary responses
Most commonly abused in health care professionalsHeroin, morphine, oxycodone, meperidine andfentanyl
This route is associated with rapid tolerance and psychologicdependence
IV administration
Leads to respiratory depression progressing to coma and death Overdose of opioids
Lacrimation, rhinorrhea, yawning, sweating, weakness,gooseflesh, nausea, and vomiting, tremor, muscle jerks, andhyperpnea are signs of this syndrome
Abstinence syndrome
Treatment for opioid addiction Methadone, followed by slow dose reductionThis agent may cause more severe, rapid and intensesymptoms to a recovering addict
Naloxone
Sedative-Hypnotics actionReduce inhibition, suppress anxiety, andproduce relaxation
Additive effects when Sedative-Hypnotics used in combinationwith these agents
CNS depressants
Common mechanism by which overdose result in deathDepression of medullary and cardiovascularcenters
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"Date rape drug" Flunitrazepam (rohypnol)
The most important sign of withdrawal syndrome Excessive CNS stimulation (seizures)
Treatment of withdrawal syndrome involvesLong-acting sedative-hypnotic or a gradualreduction of dose, clonidine or propranolol
These agents are CNS depressants Ethanol, Barbiturates, and Benzodiazepines
Withdrawal from this drug causes lethargy, irritability, andheadache
Caffeine
W/D from this drug causes anxiety and mental discomfort Nicotine
Treatments available for nicotine addictionPatches, gum, nasal spray, psychotherapy, andbupropion
Chronic high dose abuse of nicotine leads toPsychotic state, overdose causes agitation,restlessness, tachycardia, hyperthermia,hyperreflexia, and seizures
Tolerance is marked and abstinence syndrome occurs Amphetamines
Amphetamine agents Dextroamphetamines and methamphetamine
These agents are congeners of Amphetamine DOM, STP, MDA, and MDMA "ecstasy"" "
Overdoses of this agent with powerful vasoconstrictive actionmay result in fatalities from arrhythmias, seizures, respiratorydepression, or severe HTN (MI and stroke)
Cocaine "super-speed"""
Most dangerous of the currently popular hallucinogenic drugs,OD leads to nystagmus, marked hypertension, and seizures,presence of both horizontal and vertical nystagmus ispathognomonic
PCP
Removal of PCP may be aidedUrinary acidification and activated charcoal orcontinual nasogastric suction
THC is active ingredient, SE's include impairment ofjudgment, and reflexes, decreases in blood pressure and
psychomotor performance occur
Marijuana
This agent has greater affinity for muscarinic receptors andused for postoperative and neurogenic ileus and urinaryretention
Bethanechol
Only direct acting agent that is very lipid soluble and used inglaucoma
Pilocarpine
This agent used to treat dry mouth in Sjgren's syndrome Cevimeline
Indirect-Acting ACh Agonist, alcohol, short DOA and used indiagnosis of myasthenia gravis
Edrophonium
Carbamate with intermediate action, used for+A1170postoperative and neurogenic ileus and urinary retention Neostigmine
Treatment of atropine overdose and glaucoma (because lipidsoluable). Enters the CNS rapidly and has a stimulant effect,which may lead to convulsions
Physostigmine
Treatment of myasthenia gravis Pyridostigmine
Antiglaucoma organophosphate Echothiophate
Associated with an increased incidence of cataracts in patientstreated for glaucoma
Long acting cholinesterase inhibitors
Scabicide organophosphate Malathion
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Organophosphate anthelmintic agent with long DOA Metrifonate
Toxicity of organophosphate:
DUMBELSS (diarrhea, urination, miosis,bronchoconstriction, excitation of skeletalmuscle and CNS, lacrimation, salivation, andsweating)
The most frequent cause of acute deaths in cholinesteraseinhibitor toxicity
Respiratory failure
The most toxic organophosphate Parathion
Treatment of choice for organophosphate overdose Atropine
This agent regenerates active cholinesterase and is a chemicalantagonist used to treat organophosphate exposure
Pralidoxime
Prototypical drug is atropine Nonselective Muscarinic Antagonists
Treat manifestations of Parkinson's disease and EPS Benztropine, trihexyphenidyl
Treatment of motion sickness Scopolamine, meclizine
Produce mydriasis and cycloplegia Atropine, homatropine,C1208 tropicamide
Bronchodilation in asthma and COPD Ipratropium
Reduce transient hyper GI motility Dicyclomine, methscopolamineCystitis, postoperative bladder spasms, or incontinence Oxybutynin, dicyclomine
Toxicity of anticholinergicsblock SLUD (salivation, lacrimation, urination,defecation
Another pneumonic for anticholinergic toxicity"dry as a bone, red as a beet, mad as a hatter,hot as a hare, blind as a bat"
Atropine fever is the most dangerous effect and can be lethalin this population group
Infants
Contraindications to use of atropineInfants, closed angle glaucoma, prostatichypertrophy
Limiting adverse effect of ganglion blockade that patientsusually are unable to tolerate
Severe hypertension
Reversal of blockade by neuromuscular blockers Cholinesterase inhibitors
Tubocurarine is the prototype, pancuronium, atracurium,vecuronium are newer short acting agent, produce competitiveblock at end plate nicotinic receptor, causing flaccid paralysis
Nondepolarizing Neuromuscular Blockers
Only member of depolarizing neuromuscular blocker, causesfasciculation during induction and muscle pain after use; hasshort duration of action
Succinylcholine
Chemical antagonists that bind to the inhibitor of ACh Estraceand displace the enzyme (if aging has not occurred) Cholinesterase regenerators, pralidoxime
Used to treat patients exposed to insecticides such as parathion Pralidoxime, atropine
Pneumonic for beta receptors You have 1 heart (Beta 1) and 2 lungs (Beta 2)
This is the drug of choice for anaphylactic shock Epinephrine
Phenylisopropylamines that are used legitimately and abusedfor narcolepsy, attention deficit disorder, and weight reduction
Amphetamines
Alpha agonist used to produce mydriasis and reduceconjunctival itching and congestion caused by irritation orallergy, it does not cause cycloplegia
Phenylephrine
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Newer alpha 2 agonist (apraclonidine and brimonidine) treatglaucoma by acting to
Reduce aqueous secretion
Short acting Beta 2 agonists that is drug of choice in treatmentof acute asthma but not recommended for prophylaxis
Albuterol
Longer acting Beta 2 agonist is recommended for prophylaxisof asthma
Salmeterol
These agents increase cardiac output and may be beneficial intreatment of acute heart failure and some types of shock
Beta1 agonists
These agents decrease blood flow or increase blood pressure,are local decongestants, and used in therapy of spinal shock(temporary maintenance of blood pressure which may helpmaintain perfusion
Alpha1 agonists
Shock due to septicemia or myocardial infarction is madeworse by
Increasing afterload and tissue perfusiondeclines
Epinephrine is often mixed with a local anesthetic to Reduce the loss from area of injection
Chronic orthostatic hypotension can be treated with Midodrine
Beta 2 agonist used to suppress premature labor, but cardiac
stimulatory effects may be hazardous to mother and fetus
Terbutaline
Sympathetic agent which stimulates heart rate and can dilatevessels in skeletal muscle at low doses
Epinephrine
Mast cells to reduce release of hisamine and inflammatorymediators
Epinephrine
Agent used in shock because it dilates coronary arteries andincreases renal blood flow
Dopamine
Agent which stimulates cardiac contractile force more than ratewith little effect on total peripheral resistance
Dobutamine
Long acting sympathomimetic, sometimes used to improve
urinary continence in children and elderly with enuresis EphedrineAlpha 1 agonist toxicity Hypertension
Beta 1 agonist toxicity Sinus tachycardia and serious arrhythmias
Beta 2 agonist toxicity Skeletal muscle tremor, tachycardia
The selective agents loose their selectivity at high doses
Nonselective alpha-blocking drug, long acting and irreversible,and used to treat pheochromocytoma. Blocks 5-HT, sooccasionaly used for carcinoid tumor. Blocks H1 and used inmastocytosis
Phenoxybenzamine
Nonselective alpha-blocking drug, short acting and reversible,used for rebound HTN from rapid clonidine withdrawal, andRaynaud's phenomena
Phentolamine
Selective Alpha 1 blocker used for hypertension, BPH, maycause first dose orthostatic hypotension
Prazosin, terazosin, doxazosin
Selective Alpha-1A blocker, used for BPH, but with littleeffect on HTN
Tamsulosin
Selective Alpha 2 blocker used for impotence (controversialeffectiveness)
Yohimbine
SelectiveB1 Receptor blockers that may be useful in treating
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patients even though they have asthmaAcebutolol, atenolol, esmolol, metoprolol
Combined alpha and beta blocking agents that may haveapplication in treatment of CHF
Labetalol and carvedilol
Beta blockers partial agonist activity (intrinsicsympathomimetic activity) cause some bronchodilation andmay have an advantage in treating patients with asthma
Pindolol and acebutolol
This beta blocker lacks local anesthetic activity (a property
which decreases protective reflexes and increases the risk ofcorneal ulceration) and used in treating glaucoma Timolol
This parenteral beta blocker is a short acting (minutes) Esmolol
This beta blocker is the longest acting Nadolol
These beta blockers are less lipid soluble Acebutolol and atenolol
This beta blocker is highly lipid soluble and may account forside effects such as nightmares
Propranolol
Clinical uses of these agents include treatment of HTN, angina,arrhythmias, chronic CHF, and selected post MI patients
Beta blockers
Toxicity of these agents include bradycardia, AV blockade,exacerbation of acute CHF; signs of hypoglycemia may bemasked (tachycardia, tremor, and anxiety)
Beta blockers
Cholinomimetics that increase outflow, open trabecularmeshwork, and cause ciliary muscle contraction
Pilocarpine, carbachol, physostigmine
Nonselective alpha agonists that increases outflow, probablyvia the uveoscleral veins
Epinephrine, dipivefrin
Selective alpha agonists that decreases aqueous secretion Apraclonidine, brimonidine
These Beta blockers decrease aqueous secretion Timolol (nonselective), betaxolol (selective)
This diuretic decreases aqueous secretion due to lack of
HCO3- ion. Causes drowsiness and paresthesias, alkalinizationof the urine may precipitate calcium salts, hypokalemia,acidosis
Acetazolamide
This agent cause increased aqueous outflow Prostaglandin PGF2a
Inhibit angiotensin-converting enzyme (ACE) ACE inhibitors
Captopril and enalapril (-OPRIL ending) are ACE inhibitors
SE of ACE inhibitors Dry cough, hyperkalemia
ACE inhibitors are contraindicated in pregnancy and with K+
Losartan and valsartan block Angiotensin receptor
Angiotensin receptor blockers do NOT cause Dry coughAgents that block L-type calcium channel Calcium channel blockers
CCB contraindicated in CHF Verapamil
CCB with predominate effect on arteriole dilation Nifedipine
SE of CCB Constipation, edema, and headache
Agents that reduce heart rate, contractility, and O2 demand Beta-blockers
B-blockers that are more cardioselective Beta-1 selective blockers
Cardioselective Beta 1-blockers Atenolol, acebutolol, and metoprolol
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Beta-blockers should be used cautiously inAsthma (bronchospastic effects), diabetes(block signs of hypoglycemia) and peripheralvascular disease
Non-selective Beta-blocker also used for migraine prophylaxis Propranolol
SE of beta blockersBradycardia, SEXUAL DYSFUNCTION,decrease in HDL, and increase in Triglycerols(TG)
Alpha 1selective blockers
Prazosin, terazosin and doxazosin (-AZOSIN
ending)Non-selective Alpha1blockers use to treat pheochromocytoma Phenoxybenzamine
For rebound HTN from rapid clonidine withdrawal Phentolamine
A1a-selective blocker with no effects on HTN used for BPH Tamsulosin (Flomax)
SE of alpha blockersOrthostatic hypotension (especially with firstdose) and reflex tachycardia
Presynaptic Alpha 2 agonist used in HTN, and acts centrally Clonidine, and methyldopa
SE of methyldopa Positive Coomb's test, depression
Methyldopa is contraindicated in Geriatrics due to its CNS (depression) effects
SE of clonidine Rebound HTN, sedation, dry mouth
Direct vasodilator of arteriolar smooth muscle Hydralazine
SE of hydralazine Lupus-like syndrome
Arterial vasodilator that works by opening K+ channels Minoxidil
SE of minoxidil Hypertrichosis
IV Drug used Hypertensive Crisis Nitroprusside
Nitroprusside vasodilates Arteries and veins
Toxicity caused by nitroprusside and treatmentCyanide toxicity treated with sodium
thiosulfateCarbonic anhydrase inhibitor Acetazolamide
Diuretic used for mountain sickness and glaucoma Acetazolamide
SE of acetazolamide
Paresthesias, alkalization of the urine (whichmay ppt. Ca salts), hypokalemia, acidosis, andencephalopathy in patients with hepaticimpairment
MOA of loop diuretics inhibits Na+/K+/2Cl- cotransport
Site of action of loop diuretics Thick ascending limb
SE of loop (furosemide) diuretics Hyperuricemia, hypokalemia and ototoxicity
Aminoglycosides used with loop diuretics potentiate adverseeffect
Ototoxicity
Loops lose and thiazide diuretics retain Calcium
MOA of thiazide diuretics Inhibit Na+/Cl- cotransport
Site of action of thiazide diuretics Work at early distal convoluted tubule
Class of drugs that may cause cross-sensitivity with thiazidediuretics
Sulfonamides
SE of thiazide (HCTZ) diureticsHyperuricemia, hypokalemia andhyperglycemia
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Potassium sparing diuretics inhibit Na+/K+ exchange
Diuretic used to treat primary aldosteronism Spironolactone
SE of spironolactone Gynecomastia hyperkalemia, and impotence
Osmotic diuretic used to treat increased intracranial pressure Mannitol
ADH agonist used for pituitary diabetes insipidus Desmopressin (DDAVP)
Used for SIADH Demeclocycline
SE of demeclocyclineBone marrow and teeth discoloration forchildren under 8 years of age
MOA of class I A (eg. Procainamide), class IB (eg.Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
Sodium channel blockers
SE of procainamide Lupus-like syndrome
Limiting side effect of Quinidine Prolongs QT interval
Other side effects of QuinidineThrombocytopenic purpura, andCINCHONISM
Major drug interaction with Quinidine Increases concentration of Digoxin
DOC for management of acute ventricular arrhythmias Amiodarone
DOC for digoxin induced arrhythmias Phenytoin
Class of anti-arrhythmics that has a pro-arrhythmic effect(CAST trial), therefore are used as last line agents
Class IC (flecainide, propafenone, moricizine)
Class II antiarrhythmics are B-blockers
Antiarrhythmic that exhibits Class II and III properties Sotalol
Side effect of sotalol prolongs QT and PR interval
Used intravenously for acute arrhythmias during surgery Esmolol
Anti-arrhythmics that decrease mortality B-blockers
MOA of class III antiarrhythmics Potassium channel blockers
Class III antiarrhythmic that exhibits properties of all 4 classes Amiodarone
Specific pharmacokinetic characteristic of amiodarone Prolonged half-life, up to six weeks
Antiarrhythmic effective in most types of arrhythmia Amiodarone
SE of AmiodaroneCardiac dysfunction, photosensitivity, skin(blue smurf syndrome), Pulmonary fibrosis,thyroid and corneal deposits
MOA of class IV antiarrhythmics Calcium channel blockers
Life threatening cardiac event that prolong QT leads to Torsades de pointes
Agent to treat torsades de pointes Magnesium sulfate
Drug used supraventricular arrhythmias Digoxin
DOC for paroxysmal supraventricular tachycardia (PSVT) Adenosine
Adenosine's MOAActivattion on an inward K+ current andinhibition of Ca++ current resulting in markedhyperpolarization
Anti-arrhythmic with 15 second duration of action Adenosine
MOA of sildenafil (Viagra)Inhibits phosphodiesterase-5, enhancing effectsof nitric oxide-activated increases in cGMP
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Drugs used in the management of angina Aspirin, Nitrates, CCB, and Beta blockers
Aspirin reduces mortality in unstable angina by Platelet aggregation inhibition
MOA of nitratesRelax vascular smooth muscle, at low dosesdilate veins and at high doses dilate arterioles
Nitrate used for acute anginal attacks Nitroglycerin sublingual tablets
Nitrate used to prevent further attacks Oral and transdermal forms of nitroglycerin
Nitrate free intervals are needed due to Tolerance
SE of nitratesPostural hypotension, reflex tachycardia, hotflashes, and throbbing headache due tomeningeal artery dilation
CCB are DOC for Prinzmetal's angina
Beta blockers are used for which type of anginal attack Classic
MOA of Cardiac glycosides (eg. digoxin)Indirectly increase intracellular calcium andcardiac contractility by inhibiting Na+/K+ATPase
Digoxin is used in Atrial fibrillation and CHF
Digoxin toxicity can be precipitated by Hypokalemia
Antidote for digoxin toxicity Digibind
Phosphodiesterase inhibitors that increase mortality and havebeen found to have NO beneficial effects
Amrinone and milrinone
SE of amrinone Thrombocytopenia
Beta 1 agonists used in acute CHF Dobutamine and dopamine
Diuretics work in CHF by Reducing preload
Beta blockers work in CHF byReducing progression of heart failure (neveruse in acute heart failure)
Peptide drug used to treat CHF Nesiritide (BNP)MOA of nesiritide
Increasing sodium excretion and decreasesarterial and venous tone
SE of nesiritide Excessive hypotension and kidney failure
Agent used in CHF that is a selective alpha and nonselectivebeta blocker
Carvedilol
Agent used in acutely decompensated CHF resemblingnatriuretic peptide
Nesiritide (Natrecor)
Vitamin K dependent anticoagulant Warfarin (PT)
Warfarin is contraindicated in Pregnancy
Anticoagulant of choice in pregnancy Heparin
Heparin (PTT) increases activity of Antithrombin 3
Route of administration of warfarin Oral
Routes of administration of heparin IV and IM (only LMW)
SE of both warfarin and heparin Bleeding
SE of heparin Heparin induced thrombocytopenia (HIT)
Alternative anticoagulant used if HIT develops Lepirudin
Antidote to reverse actions of warfarin Vitamin K or fresh frozen plasma
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Antidote to reverse actions of heparin Protamine sulfate
MOA of aspirin Irreversibly blocking cyclooxygenase
Agent used to treat MI and to reduce incidence of subsequentMI
Aspirin, metoprolol
SE of Aspirin GI bleeding
Antiplatelet drug reserved for patients allergic to aspirin Ticlopidine
SE for ticlopidine Neutropenia and agranulocytosis
Effective in preventing TIA's Clopidogrel and ticlopidinePrevents thrombosis in patients with artificial heart valve Dipyridamole
Block glycoprotein IIb/IIIa involved in platelet cross-linking Abciximab, tirofiban and eptifibatide
MOA of thrombolyticsDegradation of fibrin clots and areadministered IV
Thrombolytics are used for Pulmonary embolism and DVT
Thrombolytic that can cause allergic reaction Streptokinase
Thrombolytic used for acute MI and ischemic (nonhemorrhagic) CVA
Tissue plasmin activator
SE of tPA Cerebral hemorrhageAntidote for thrombolytics Aminocaproic acid
Agent to treat hypochromic microcytic anemias Ferrous sulfate
Chelating agent used in acute iron toxicity Deferoxamine
Agent for pernicious anemia Cyanocobalamin (Vit B12)
Agent used for neurological deficits in megaloblastic anemia Vitamin B12
Agent used for megaloblastic anemia (but does NOT reverseneurologic symptoms) and decrease neural tube defects duringpregnancy
Folic acid
Agent used for anemias associated with renal failure Erythropoietin
Agent used neutropenia especially after chemotherapyG-CSF (filgrastim) and GM-CSF(sargramostim)
Treatment of patients with prior episodes of thrombocytopeniaafter a cycle of cancer chemotherapy
Interleukin 11 (oprelvekin)
Drugs decrease intestinal absorption of cholesterol Bile acid-binding resins
Cholestyramine and colestipol are Bile acid-binding resins
Major nutritional side effect of bile acid-binding resinsImpair absorption of fat soluble vitaminabsorption (A,D,E,K)
MOA of lovastatin (STATIN) inhibits HMG COA reductaseHMG CoA reductase inhibitors are contraindicated in Pregnancy
MOA of drug or foods (grapefruit juice) that increase statineffect
Inhibit Cytochrome P450 3A4
SE of HMG COA reductase inhibitors Rhabdomyolysis and Hepatotoxicity
Monitoring parameter to obtain before initiation of STATINS LFT's
Decreases liver triglycerol synthesis Niacin
SE of niacin Cutaneous flush
Cutaneous flush and be reduced by pretreatment with Aspirin
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Fibrates (gemfibrozil) increase activity of Lipoprotein lipase
Most common SE of fibrates Nausea
Fibrates are contraindicated in Pregnancy
Concurrent use of fibrates and statins increases risk of Rhabdomyolysis
New class of drugs that works by inhibiting absorption ofintestinal cholesterol and can be given concurrently with theStatins
Ezetimibe (Zetia)
MOA of NSAIDS inhibit prostaglandin synthesis by inhibitingcyclo-oxygenase (cox)
Difference between aspirin and other NSAIDS Aspirin irreversibly inhibits cyclooxygenase
Four main actions of NSAIDSAnti-inflammatory, analgesia, antipyretic andantiplatelet activity
Agent used for closure of patent ductus arteriosus Indomethacin
Aspirin is contraindicated in children with viral infection Potential for development of Reye's syndrome
SE of salicylates Tinnitus, GI bleeding
NSAID also available as an ophthalmic preparation Diclofenac, ketoralac
NSAID available orally, IM and ophthalmically KetoralacNSAID that is used for acute condition, such as pre-opanesthesia and has limited duration (
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NSAID used in gout Indomethacin
NSAID contraindicated in gout Aspirin
MOA of colchicine (used in acute gout) Selective inhibitor of microtubule assembly
SE of colchicine Kidney and liver toxicity, diarrhea
Agent used to treat chronic gout by increasing uric acidsecretion and excretion
Probenecid and sulfinpyrazone
Allopurinol treats chronic gout by decreasing uric acid
production by inhibitingXanthine oxidase
Rapid acting insulins that do not self-aggregate lispro insulin, aspart insulin, glulisine insulin
Peakless ling acting insulin Insulin glargine
DOC for paroxysmal supraventricular tachycardia; has highefficacy and short duration of action
Adenosine
Insulin bound to neutral protamine NPH (NP = neutral protamine)
Insulin that self-aggregates into hexamers insulin glargine
Side effect of quinidine characterised by tinnitus, headache,deafness, and (occasionally) anaphylactoid shock
Cinchonism
This antibiotic can be used to treat Paget's disease of bone aswell as hypercalcemia plicamycin