VANCOMYCIN

VANCOMYCIN HYDROCHLORIDE

By: Komal Haleem, Pharm-D

•Vancomycin is a glycopeptide antibiotic used in the prophylaxis and treatment of infections caused by Gram-positive bacteria.

•Vancomycin is used to treat infections of the intestines that cause colitis (inflammation of the large intestine).

DESCRIPTION

BRAND NAMES

VANCOCIN

ELI LILLY PAKISTAN (PVT)

LTD.

VANCOMYCIN

ABBOTT LABORATORIES (PAKISTAN) LIMITED.

PREPARATIONS

125 mg

250mg

500 mg

750mg

1g

5g

10g

- Capsules, oral

- Injection, lyophilized powder for solution:

- Injection, frozen, premixed solution:

500 mg per 100 mL

750 mg per 150 mL

1 g per 200 mL

INDICATIONS AND USAGE

ORAL

• Treatment of Clostridium difficile –associated diarrhea

• Treatment of staphylococcal enterocolitis.

PARENTERAL

• Treatment of serious or severe infections caused by susceptible strains of methicillin-resistant (beta-lactam–resistant) staphylococci

• Treatment of staphylococcal, streptococcal, enterococcal, or diphtheroid endocarditis.

UNLABELLED USES

Aerosolization

Central venous catheter infection

Preoperative prophylaxis

Rectal administration

Ventricular shunt infections.

Inhibits cell wall synthesis.

Inhibits transglycosylase.

Alters cell membrane permeability.

Cell becomes susceptible to lysis.

MECHANISM OF ACTION

MECHANISM OF ACTION

PHARMACOKINETICS

ADME

ABSORPTION

Poorly absorbed (orally).

When given by injection:

• C max is 63 mcg/mL

• T max is 1 h (injection)

DISTRIBUTION

55% protein bound.

Vd is 0.3 to 0.43 L/kg.

Distributes in:

• Pleural fluid

• Pericardial fluid

• Ascitic fluid

• Synovial fluid

• Urine

• Peritoneal dialysis fluid

• Atrial appendage tissue

No apparent metabolism of the drug.

IV: about 75% is excreted in the urine by

glomerular filtration (in the first 24 hrs).

Mean half-life is 4 to 6 hrs.

Oral: feces

SPECIAL POPULATIONS

RENAL FUNCTION IMPAIREMENT:

Slows excretion of vancomycin

In anephric patients: half-life is 7.5 days.

Dosage adjustment is required.

ELDERLY:

Total systemic and renal Cl may be reduced.

Dosage adjustment is required.

DOSAGE

Endocarditis (staphylococcal, streptococcal,

enterococcal, diphtheroid), staphylococcal

infections

IV 500 mg every 6 h or 1 g every 12 h at a rate no faster than 10 mg/min or over at least 60 min, whichever is longer.

IV 10 mg/kg per

dose given every 6

h over at least 60

min.

IV initial dose of 15

mg/kg, followed by 10

mg/kg every 12 h in the

first week of life and

every 8 h thereafter up

to 1 month of age.

C. difficile –associated diarrhea

PO 125 mg 4 times daily for

10 days.

PO 40 mg/kg/day in 3 or 4

divided doses for 7 to 10

days; max dosage is 2 g/day.

Staphylococcal enterocolitis

PO 500 mg to 2 g in 3 or 4

divided doses for 7 to 10

days.

PO 40 mg/kg/day in 3 or 4

divided doses for 7 to 10

days

ADVERSE REACTIONS

Cardiovascular

Hypotension.

CNS

Headache, fatigue, dizziness, vertigo (rare).

Dermatologic

Drug rash, exfoliative dermatitis, pruritus, Stevens-

Johnson syndrome, urticaria, vasculitis.

Hematologic

Reversible agranulocytosis; eosinophilia,

thrombocytopenia

ENT

Hearing loss; tinnitus (rare).

GI

Nausea; abdominal pain; diarrhea, vomiting; flatulence; antibiotic-associated colitis.

Genitourinary

UTI; nephrotoxicity including increased blood creatinine, renal failure, and renal impairment

Local

Injection-site inflammation.

Respiratory

Dyspnea, wheezing.

Red man syndrome

Flushing of the face, neck, upper chest,

and extremities

Hypokalemia

Pyrexia

PRECAUTIONS

Pregnancy

Category C (injection); Category B (oral).

Lactation

Excreted in breast milk.

Renal Function

Dosage adjustments required; use with caution.

Children

Confirming serum levels is recommended.

Elderly

Adjust dosage schedules.

Administration

Give by secure IV route. May minimize thrombophlebitis by giving slowly as dilute infusion.

CONTRAINDICATIONS

Hypersensitivity to vancomycin

Hypersensitivity to corn

or corn products.

OVERDOSAGE

Hearing loss,

increased BUN,

increased serum creatinine,

ringing in ears,

vertigo.

DRUG INTERACTIONS

ANESTHETICS

• increased risk of hypersensitivity & infusion-related reactions

INDOMETHACIN • increases vancomycin toxicity in neonates.

METHOTREXATE• increases methotrexate toxicity

NON DEPOLARIZING MUSCLE RELAXANTS

• neuromuscular blockade may be enhanced

AMINOGLYCOSIDES, AMPHOTERICIN B,

BACITRACIN, CISPLATIN, POLYMIXIN B

• increases risk of nephrotoxicity and/or neurotoxicity.

Storage & Stability

Parenteral

Store vials at 68° to 77°F.

After reconstitution,

vials may be stored in a

refrigerator for 14 days.

Oral

Store at 59° to 86°F.

PATIENT COUNSELING

Explain that IV medication is given at regular intervals to maintain blood levels.

Tell patients to report hearing loss, ringing in ears, or vertigo to their health care provider.

Identify symptoms of potential adverse reactions.

Tell patients to maintain adequate fluid intake.

Tell patients not to stop taking vancomycin, even if they start tofeel better.

PREDNISONE

Prednisone is a corticosteroid. It prevents the release

of substances in the body that cause inflammation.

Prednisone also suppresses the immune system.

Prednisone is used as an anti-inflammatory or an

immunosuppressant medication

DESCRIPTION

BRAND NAMES

Prednisone Tablet

Watson Laboratories, Inc.

FORTIPRED

REMINGTON

PHARMACEUTICAL

INDUSTRIES (PVT) LTD.

INDICATIONS AND USAGE

1. Endocrine disorders;

2. rheumatic disorders;

3. collagen diseases;

4. dermatologic diseases;

5. allergic and inflammatory ophthalmic processes;

6. respiratory diseases;

7. hematologic disorders;

8. neoplastic diseases;

9. edematous states (because of nephrotic syndrome);

10. GI diseases;

11. tuberculous meningitis;

12. trichinosis with neurologic or myocardial involvement.

UNLABELLED USES

COPD;

Duchenne muscular dystrophy;

Graves ophthalmopathy.

PHARMACOLOGY

Intermediate-acting glucocorticoid

that depresses formation, release, and

activity of endogenous mediators of

inflammation, including

prostaglandins, kinins, histamine,

liposomal enzymes, and complement

system.

Also modifies body's immune

response.

PHARMACOKINETICS

ADME

Absorption

Rapid, almost complete.

Distribution

Crosses placenta.

Metabolism

Mainly hepatic, also renal and in the tissue. Prednisone is inactive and rapidly metabolized to active prednisolone.

Elimination

Renal. Plasma t ½ is 3.4 to 3.8 h.

Peak

1 to 2 h.

Duration

1.25 to 1.5 days.

DOSAGE

Adults

PO 5 to 60 mg/day.

COPD Adults

PO 30 to 60 mg/day for 1 to 2 wk, then taper.

Duchenne Muscular Dystrophy Adults

PO 0.75 to 1.5 mg/kg/day.

Graves Ophthalmopathy Adults

PO 60 mg/day; taper to 20 mg/day.

CONTRAINDICATIONS

Systemic fungal infections

administration of

live virus vaccines.

DRUG INTERACTIONS

Anticholinesterases

Antagonizes anticholinesterase effects in myasthenia gravis.

Anticoagulants, oral

Alters anticoagulant dose requirements.

Barbiturates, hydantoins (eg, phenytoin), rifampin

Decreased pharmacologic effect of prednisone.

Cyclosporine

Enhanced cyclosporine toxicity.

Estrogens, ketoconazole,

oral contraceptives

Decreased Cl of prednisone.

Nondepolarizing muscle relaxants

May potentiate, counteract, or have no effect on

neuromuscular blocking action.

Salicylates

Reduced serum levels and efficacy of salicylates.

Somatrem

Inhibition of growth-promoting effects of somatrem.

Theophylline

Alterations in pharmacologic activity of either agent.

ADVERSE REACTIONS

Cardiovascular

Thromboembolism or fat embolism; thrombophlebitis; cardiac

arrhythmias or ECG changes; hypertension; myocardial rupture;

CHF.

CNS

Convulsions; pseudotumor cerebri; vertigo; headache;

psychosis.

Dermatologic

Impaired wound healing; thin fragile skin; erythema; lupus

erythematosus-like lesions; subcutaneous fat atrophy; purpura;

hirsutism; acneiform eruptions; allergic dermatitis; urticaria;

angioneurotic edema

EENT

Posterior subcapsular cataracts; increased IOP; glaucoma;

exophthalmos.

Genitourinary

Increased or decreased motility and number of spermatozoa.

Hematologic

Leukocytosis.

Metabolic

Sodium and fluid retention; hypokalemia; hypokalemicalkalosis; metabolic alkalosis; hypocalcemia.

GI

Pancreatitis; abdominal distention; ulcerative esophagitis; nausea; vomiting; increased appetite and weight gain; peptic ulcer with perforation and hemorrhage; small and large bowel perforation.

PRECAUTIONS

Pregnancy

Category C .

Lactation

Children

Elderly

Renal Function

Hypersensitivity

Adrenal suppression

Cardiovascular effects

Hepatitis

Immunosuppression

Infections

Ocular effects

Use systemic drug cautiously in ocular herpes simplex because of possible corneal perforation.

Ophthalmic use

Peptic ulcer

Stress

Withdrawal

Abrupt discontinuation may result in adrenal insufficiency.

OVERDOSAGE

Cushingoid changes, Moonfaced, central obesity

hirsutism, acne, ecchymoses, hypertension,

osteoporosis, myopathy

sexual dysfunction

diabetes mellitus, hyperlipidemia

peptic ulcer, GI bleeding

increased susceptibility to infection

electrolyte and fluid imbalance

psychosis

VENTOLIN S.R

(SULBUTAMOL BP)

DESCRIPTION

Salbutamol tablets belong to a group of medicines called

selective beta-2-adrenergic agonists, which can be used to

relax the muscles of the airways.

Salbutamol is available for administration by the following

routes:Inhalation, tablet, elixir, intravenous injection,

subcutaneous injection,intramuscular injection

INDICATIONS

Salbutamol is a beta-adrenergic stimulant which has a highly

selective action on beta2-receptors in bronchial smooth muscle

and in therapeutic dosage, little or no action on cardiac beta1-

receptors.

Salbutamol has an advantage in asthma treatment by

minimising side effects associated β1 receptor stimulation

•Asthma, to relieve the narrowing of the airways

•Chronic bronchitis

•Emphysema

•Prevention of premature labour.

USAGE

Pharmacokinetics

Absorption

DISTRIBUTION

Salbutamol binds to and releases from plasma

proteins as necessary.

METABOLISM

Salbutamol absorbed in the gastrointestinal tract

has a substantial first pass metabolism and is

metabolized into Phenolic Sulfate.

Inhaled Salbutamol acts directly on smooth

muscle of the upper airways bypassing

metabolism in the liver.

EXCRETION

Excretion

Salbutamol and Phenolic Sulfate are primarily

excreted via the urinary system.

DOSAGE AND ADMINISTRATION

Ventolin S.R. Tablets must be swallowed whole with a glass of

water and not chewed or crushed.

Adults:

Usual dose is 4mg three or four times a day. Your doctor may

increase this gradually up to a maximum of 8mg three or four

times a day. Some patients may be treated successfully with

2mg three or four times a day.

Children 2-6 years:

1-2mg three or four times a day.

Children 6-12 years:

2mg three or four times a day.

Children over 12 years:

2-4mg three or four times a day.

Children under 2 years:

Not recommended.

Premature labour:

The maintenance dose is 4mg three or four times a day.

DOSAGE AND ADMINISTRATION

CONTRA-INDICATIONS

Ventolin oral preparations are contra-indicated in patients with

a history of hypersensitivity to any of their components.

Intravenous salbutamol and occasionally salbutamol tablets are

used in the management of premature labour uncomplicated by

conditions such as placenta praevia, antepartum heamorrhage

or toxaemia of pregnancy.

Salbutamol presentation should not be used for threatened

abortion.

WARNINGS

Increase use of short-acting inhaled beta2-agonists to control

symptoms indicates deterioration of asthma control.

Sudden and progressive deterioration in asthma control is

potentially life-threatening and consideration should be given

to starting or increasing corticosteroid therapy.

If dose fails to give usual relief, medical advice should be

sought.

PRECAUTIONS

Salbutamol and non-selective beta-blocking drugs, such as

propranolol, should not usually be prescribed together.

Salbutamol should be administrated cautiously to the patients

suffering from thyrotoxicosis.

Particular caution is advised in acute severe asthma, as this

effect may be potentiated by concomitant treatment with

xanthine derivatives, steroids, diuretics and by hypoxia.

Administration of drugs during pregnancy should

only be considered if the expected benefit to the

mother is greater than any possible risk to the fetus.

PREGNANCY

Salbutamol is probably secreted in breast milk, its

use in nursing mothers is not recommended unless

the expected benefits outweigh any potential risk. It

is not known whether salbutamol in breast milk has

a harmful effect on the neonate.

LACTATION

SIDE EFFECTS

Ventolin oral preparations may cause a fine tremor of

skeletal muscle in some patients.

Occasionally headaches.

Feeling of tension in some patients.

Hypersensitivity reactions including angioedema,

urticaria, bronchospasm, hypotension and collapse have

been reported very rarely.

An allergic reaction (hypersensitivity): swelling of the face, lips,

throat or tongue, pale or red irregular raised patches with severe

itching (hives), difficulty breathing, low blood pressure, collapse.

Increased lactic acid in the body: rapid breathing, being sick,

stomach pain.

Low blood potassium: muscle twitching or weakness, an irregular

heart beat.

SIDE EFFECTS

Salbutamol is not contra-indicated in patients

under treatment with monoamine oxidase

inhibitors ( MAOIs).

DRUG INTERACTIONS

OVER DOSAGE

Antidote for over dosage with salbutamol is a

cardio-selective beta blocking agent.

•Storage :

Below 30˚C

•Don’t remove frompack until required.

PHARMACEUTICAL

PRECAUTIONS