clinical pharmacology tbmm frida
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CLINICAL PHARMACOLOGY
DRUG PRESCRIPTION DIKLAT RUANG TBMM NURUL QOLBI
FRIDA NEILA RAHMATIKANIA. 0811010303
FARMAKOKINETIK
FARMAKODINAMIK
DRUGS
Drug Therapy Decision
Drug designed into a dosage from that can be given to a
patient
D Drug acts to produces its effect on the body
Is the effect on the body beneficial or harmful to the patient?
PharmacologyPharmaceutics
Pharmacokinetics Pharmacodynamics
Therapeutics
A EM
SystemicEnteral
© Oral© Mucous :Sublingual, buccal, nasal, vaginal, rectal
Parenteral © Injection : Intravenous(i.v), intramuscular(i.m), subcutaneous
(s.c), intraperitoneal (i.p), intra-arterial, intrathecalTopikal
©dermal, vaginal, rectal©inhalation
ROUTES OF ADMINISTRATION
The main routes of drug administration and elimination
HOW DO DRUGS WORK?
a. Act on receptors (more)b. Act on ion channel : Ca antagonists, local
anaesthetics, cardiac glycosides, c. Alter enzyme function : COX inhibitors, MAO
inhibitors, AChE inhibitorsd. Act on transporter system : Selective Serotonin
Reuptake Inhibitors, Inhibitors of Na-2Cl-K Symporter (Loop Diuretics)
e. Act on signal transduction protein: Tyrosine Kinase Inhibitors, Type 5 Phosphodiesterase Inhibitors
f. Unconventional mechanism of action
HOW DO DRUGS WORK BY UNCONVENTIONAL MECHANISMS OF ACTION?
• Disrupting of Structural Proteins e.g. vinca alkaloids for cancer, colchicine for gout
• Being Enzymese.g. streptokinase for thrombolysis
• Covalently Linking to Macromoleculese.g. cyclophosphamide for cancer
• Reacting Chemically with Small Moleculese.g. antacids
• Binding Free Molecules or Atomse.g. drugs for heavy metal poisoning, infliximab (anti-TNF)
HOW DO DRUGS WORK BY UNCONVENTIONAL MECHANISMS OF ACTION ? (cont’nd..)
• Being Nutrientse.g. vitamins, minerals
• Exerting Actions Due to Physical Propertiese.g. mannitol (osmotic diuretic), laxatives
• Working Via an Antisense Actione.g. fomivirsen for CMV retininitis in AIDS
• Being Antigens e.g. vaccines
• Having Unknown Mechanisms of Actione.g. general anesthetics
GIT DRUGS
Menghambat prod HCl
AH2• Cimetidine• Ranitidine• Famotidine• Nizatidine
ULCUS PEPTICUM
PPI• Omeprazol
e• Lansoprazole
Melindungi Mukosa
Sucralfate PG Analog• misoprost
ol
Antasida• Mg(OH)2• Al(OH)3
ANTIKONSTIPASI
Laxative
Chathartic
Bulk forming• Psyllium• Polycarbophil• Methylcellulos
e• Mak berserat
Surfactants• Docusate
salts
Stimulants/ Irritant• Bisacodyl• Anthraquinone• Danthron• Sodium
picosulfat
Osmotics• Mg(OH2)• Lactulose
ANTIDIAREOpiate-like Antidiarrheal Agent• Paregoric/ opium
tincture• Diphenoxylate• Difenoxin• Loperamide• codeine
Stool Modifiers• Kaolin• Wheat brand
Antiemetic5HT3 Antagonist• Ondansetron• Granisetron
DA Antagonist
Phenothiazines• Prochlorperazine• Promethazine
Butyrophenones• Haloperidol• droperidolMetoclopramide
Antikolinergik Cannabinoids
Tetrahydrocannabinol• Dronabinol• Nabilone
RESPIRATORY
DRUGS
bronkodilator
Early response :Bronchoconstriction
antiinflamasi
Late response :Inflamation
Hyperreactivity
TERAPI ASMAAg (polutan, alergen)
hindariAg
Ag-Ab/IgE di mast cellantiinflamasi, kromolin
MEDIATOR
Symptom
OBAT ASMA1. Bronkodilator
Β2 antagonis/Simpatomimetik/ adrenergik
Antagonis muskarinik/ M3/Antikolinergik Methylxantin
• Metaproterenol (pot >>)• Formoterol (durasi >>)• Salmeterol/ Salbutamol• Terbutaline• Adrenalin/ Epinephrine• Ephedrine
• Ipratropium bromide• Tiotropium bromide• Atropine
• Theophylline• Teobromine• Caffeine
OBAT ASMA CONT’ND...2. Antiinflamasi
Glukokortikoid Inhibitor degranulasi sel mast
Oral:• Prednisone• Betamethasone (pot, dur
>>)
• Sodium cromolyn (inh) Anti IgE:• Omalizumab
Inhalasi:• Triamcinolone• Budesonide• Fluticasone• Beclomethasone• flunisolide
OBAT ASMA CONT’ND...3. Menghambat Kerja Mediator yg Dilepaskan sel
Mast
Inhibitor Leukotrien AH1
Antagonis R/ Leukotrien (LT-1)• Zafirlukast• Montelukast
Inhibitor Lipoxygenase• Zileuton
OBAT PILEK (DEKONGESTAN)
Sistemik/ Oral Lokal/ NasalSpray: dewasaDrops: < 6 th
• Pseudoephedrine• PPA• Phenylephrine • Ephedrine 0,25%
• Naphazoline HCl 0,05%• Oxymetazoline 0,025. 0,05%• Phenylephrine• Xylometazoline HCl 0,025. 0,1%
MK: agonis R/ α – vasokonstriksi – mukosa & sekresi - hidung longgar
AH1 Gen 2• Cetirizine• Loratadin
e• Terfenadin• Astemizol
Gen 1• Diphenhydrami
ne• Chlorphenirami
ne• Promethazine• Cyproheptadin
e• Clemastine• Bisulepin• Dimetinden• Azatadin• Embramin
MK: prod sekret
OBAT BATUK
perifer central
• Uap menthol, miny. Eucaliptus
• Anestesi lokal topikal (benzocaine, lidocaine)
• Benzonatate
Opioid• Codeine• Morphine• Hydrocodon
e
MK: menekan refleks batuk
1. Antitusif
Non Opioid• DMP
(Dextromethorphan)
OBAT BATUK CONT’ND
• Guaifenesin (GG)• Menthol & Camphor• Ammonium Chloride• Ipecac• Potassium Iodide
MK: mengencerkan sekret – merangsang pengeluaran sekret
2. Ekspektoran
• N-Acetylcysteine MK: menurunkan viskositas sekret dgn merusak ik. Disulfida• DNA-ase (Pulmozyme) MK: merusak DNA mukus scr enzimatik
3. Mukolitik
OBAT ANTINYERI,
ANTI-INFLAMASI,
ANTIPIRETIK
SARAF SENSORISTransmisi
MEKANISME NYERI STIMULUS
KERUSAKAN JARINGAN
MEDIATOR NYERI(HISTAMIN,PG,BRADIKININ,LEOKOTRIEN,SEROTONIN DLL)
RESEPTOR NYERI ( (nociceptor)
MEDULA SPINAL
THALAMUS / KORTEKS PUSAT NYERI
analgesik non narkotik
NSAIDAntiinflamasi
steroid
Transduksi
Modulasi
Persepsi
anestesi lokal
Analgesik narkotik
Anestesi umum
Tx overdosis opioid
Non OpioidAcetaminophen COX-1
Inhibitor
COX-2 Inhibitor• Celecoxib• Rofecoxib• Valdecoxib
Tramadol
OBATANESTESI LOKAL
OBAT
Prokain, tetracaine, cocaineLidokainMepivacainePrilokainBupivakainRopivakain (Naropin)
%
2-4%1-2%1-2%1-2%0,5%
2,5-7,5%
DURASI
1½ jam1-2 jam1-2 jam1-2 jam5-7 jam6-8 jam
MAX
1000 mg500 mg500 mg500mg200 mg
(Levobupivakain) Chirokain
ester
amida
last
<2 hours
<4 hours
4-6 hours
6 to 72 hours
severity
mild MigraineHeadache
Moderate MigraineHeadache
Severe MigraineHeadache
Severe Refractory
over 72 hoursMigraine Headachestatus migrainosus
Obat MigraineTTT
analgesics (Aspirin,Acetaminophen , NSAIDS ) ,
Antiemeticrefractory to above
give Antiemetic , analgesics ,Triptan agents .
refractory to abovegive Other Antiemetic ,
Serotonin Agonist(Dihydroergotamine , Triptans)
refractory to aboveEmergency ttt
5HT 1D agonist
Partial agonist α & 5HT
ANTI-GOUT
ANTIHIPERTENSI
JNC 7:New Blood Pressure Classification
Blood Pressure ClassificationSBP* DBP*(mm Hg)Normal
<120 and <80Prehypertension120-139 or 80-89
Stage 1 hypertension140-159 or 90-99
Stage 2 hypertension160 or 100
Bagaimana Terapi Hipertensi ?
Terapi Non farmakologis : Life style modification
stop merokokdiet : kurangi makanan berlemak & asupan garam,tambah suplemen ion K, Ca, Mg
menurunkan BB aktivitas fisik / OR relaksasi (kurangi stress)
Terapi Farmakologis : Obat antihipertensi
Penggolongan antiHTCCB Nifedipine, verapamil, diltiazem
Vasodilator Oral
Parenteral
Melepaskan NO: hydralazine
Membuka kanal K+: minoxidil
Melepaskan NO: nitroprusside
Membuka kanal K+: diazoxide
ACEI Captopril, enalapril, quinapril, ramipril
Diuretik Thiazid: HCT (hydrochlorothiazide) chlorthalidone
Loop Diuretik: furosemide, torsemide, bumetanide
DHK+: amiloride, triamterene, spironolactone
ARB Irbesartan, losartan, valsartan
Simpatolitik agents
CNS Aktivasi reseptor α2: clonidine, guanabenz, guanfacine
Membentuk neurotransmiter palsu: methyldopa
Ganglion otonom Blok R/ Nikotinik: hexamethonium
Ujung saraf
Menghambat transpor NE ke vesikel sinaps: reserpine
Mengosongkan & memblok pelepasan NE dari tmp penyimpanannya: guanethidine
R/ Adrenergik α1 blocker: prazosin, oxazosin, terazosin
β1 blocker: atenolol, metoprolol
β blocker: propranolol
ANTIDIABETIK
PRINSIP PENATALAKSANAAN DM• Pengaturan diet
– Minum air banyak, susu skim dan minuman berkalorirendah lainnya pada waktu makan
– Hindari makanan manis, gorengan, biskuit, cake– Makanlah dengan waktu yang teratur– Tingkatkan asupan sayuran dua kali tiap makan– Jadikan nasi, roti, kentang, atau sereal sebagai menu utama– Minum air atau minuman bebas gula setiap anda haus
• Latihan jasmaniKegiatan jasmani sehari – hari dan latihan jasmani teratur, 3 –4 x/mgg, selama ± 30 menit : jalan, bersepeda santai, jogging,berenang. Latihan jasmani me BB dan memperbaikisensitifitas thd insulin, serta me uptake glukosa oleh otot(tanpa perlu bantuan insulin)
• Farmakoterapi
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Oral Antidiabetics
Ada 5 kelompok :A. SulfonylureasB. MeglitinideC. BiguanidD. GlitazoneE. Alpha-glucosidase inhibitor
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Mekanisme kerjaOral Antidiabetics (OAD)
• Me absorbsi glukosa : acarbose, biguanid• Me sekresi insulin (secretagogues) :
sulfonilurea 1st, 2nd ,3rd , meglitinide• Me produksi glukosa hepar : biguanid• Me uptake glukosa di perifer :
sulfonilurea 2nd, 3rd , biguanid, thiazolidindion
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ANTIBIOTIK
ANTIBAKTERIMenghambat sintesis dinding sel
Merusak membran plasma
Menghambat sintesis protein
• β laktam• Bacitracin (polipeptid siklik)• Glikopeptid: vancomycin, teicoplanin• Fosfomycin
• Polipeptida: tirosidin, gramisidin, polymyxin, bacitracin
• Polien: nystatin, amphotericin B
Menghambat sintesis as nukleat(Penghambat Girase/ Kuinolon)
• Aminoglikosida: 30S, 50S• Tetrasiklin: tetracycline, oxytetracycline,
chlortetracycline, rolitetracycline, demeclocycline, doxycycline, minocycline
• Linkosamid: clindamycin, lincomycin• Makrolid: erythromycin, josamycin,
spiramycin, roxithromycin, Clarithromycin
Menghambat sintesis metabolit esensial
• Sulfonamid: sulfacarbamid, sulfamethoxazole, sulfalen, sulfasalazine
• Diaminobenzilpirimidin: trimethoprim, tetroxoprim, pyrimethamine
β laktam
Penisilin
• Penisilin G (Benzilpenicillin Na/K)• Penisilin depot: benzilpenicillin-procain,
benzilpenicillin-benzatin• Penisilin oral: penicillin V (phenoxymetylpenicillin),
propycillin• Penisilin oral stabil thp B-laktamase: oxacillin,
dicloxacillin, flucoxacillin• Penisilin spektrum luas: ampicillin, amoxicillin,
bacampicillin (ester sikarboniloksietil)• Penisilin spek luas thp kuman gram (-) yg sulit
dibasmi: mezlocillin, piperacillin)• Inhibitor B-laktamase: clavulenic acid, sulbactam,
tazobactam
Sefalosporin
Karbapenem
Generasi 1: cefadroxil, cefazolin, cefalotin, cefapirin, cefradin (Gr +)
Generasi 2: cefamandole, cefumaxime, cefuroksime, cefotiam (Gr -)
Generasi 3: cefotaxime, ceftriaxone (Gr -)Generasi 4: cefepime (Gr +)
Imipenem, meropenem
Monobaktam Aztreonam
• Generasi 1 (sal kemih): nalidicid acid, pipemidat acid, norfloxacin• Generasi 2 (spek lebar): ofloxacin, ciprofloxacin• Generasi 3 (gram + & atipikal): levofloxacin, grepafloxacin, sparfloxacin• Generasi 4 (gram +, atipikal, anaerob): trovafloxacin, moxyfloxacin, clinafloxacin
Menghambat sintesis as nukleat(Penghambat Girase/ Kuinolon)
• 30S: streptomycin, neomycin, gentaycin, kanamycin, amikacin, sisomycin, tobramycin, spectinomycin
• 50S: (chloramphenicol, azidamphenicol, tiamphenicol), fusidic acid
Aminoglikosida
ANTIMIKOTIK/ ANTIFUNGALMembrane disrupting agents
Ergosterol syn inh
Nucleic acid inh
Amphotericin B, Nystatin
• Imidazol: clotrimazole, miconazole, ketoconazole• Triazol: fluconazole, itraconazole• Alilamin: naftifine• Tiokarbamat: tolnaftate• Morfolin: amorolphylline
Flucytosine
Antimitotic (spindle disruption) Griseofulvin
AntiamoebaNitroimidazol Metronidazole, tinidazole
AntiviralAntiherpes Acyclovir, valacyclovir, brivudine, famcyclovir,
idoxuridine, gancyclovir, foscarnet, cidofovir
Antifungal
Antiviral
Tablet Fe
dr. XXXXXXXX S . P : 02.01.6.1.I.034x S I P : 42x/MLG/DU/V/2002
Alamat Rumah : Jl. Melati no. X MalangPraktek : Jl. Rasuna Said 1 Malang . Telp : 348110Jam : 17.00 – 19.00
Malang, 12 – 11 – 2007
R/ Methampyron ........................ 500 mg. Diazepam ............................... 2 mg. Coffein ................................... 20 mg. Vit B1 ..................................... 50 mg.
Mf . la pulv . da in caps dtd . No . XII.S 1 dd caps . I
P . P Pro : Tn. Dody BB : Alamat : ………… Umur :
50
Inscriptio
Prescriptio
Subscriptio
Signatura
Obat Luar
PULVERES
A