๐ Indications & Clinical Dosage
*Thyrotoxicosis (adjunct):*
ORAL: Adult: 10-40 mg 3-4 times a day
*Thyrotoxic crisis:*
BY IV INJ: Adult: 1 mg, to be given over 1 minute, dose may be repeated if necessary at intervals of 2 minutes, total dose is 5mg in anaesthesia; max.10 mg per course.
*Hypertension:*
ORAL: Adult: Initially 80 mg twice daily, dose should be increased at weekly intervals as required; maintenance
160-320 mg daily.
*Prophylaxis of variceal bleeding in portal hypertension:*
ORAL: Adult: Initially 40 mg twice daily, then increased to 80 mg twice daily (max. per dose 160 mg twice daily), dose to be adjusted according to heart rate.
*Phaeochromocytoma (only with an alpha-blocker) in preparation for surgery:*
ORAL: Adult: 60 mg daily for 3 days before surgery.
*Phaeochromocytoma (only with an alpha-blocker) in patients unsuitable for surgery:*
ORAL: Adult: 30 mg daily.
*Angina:*
Adult: Initially 40 mg 2-3 times a day; maintenance 120-240 mg daily.
*Hypertrophic cardiomyopathy, Anxiety tachycardia:*
Adult: 10-40 mg 3-4 times a day.
*Anxiety with symptoms such as palpitation, sweating and tremor:*
Adult: 40 mg once daily, then increased if necessary to 40 mg 3 times a day.
*Prophylaxis after myocardial infarction:*
Adult: Initially 40 mg 4 times a day for 2-3 days, then 80 mg twice daily, start treatment 5 to 21 days after infarction.
*Essential tremor:*
Adult: Initially 40 mg 2-3 times a day; maintenance 80-160 mg daily.
*Migraine prophylaxis:*
Adult: 80-240 mg daily in divided doses.
*Arrhythmias:*
ORAL: Adult: 10-40 mg 3-4 times a day
BY IV INJ: Adult: 1 mg, to be given over 1 minute, dose may be repeated if necessary at intervals of 2 minutes, max. 10 mg per course (5mg in anaesthesia).
Children: Not recommended.
๐ Mode of Administration
IV administration should not exceed 1 mg/ min. IV dose is much smaller than oral dose.
โ Contraindications
Acute or decompensated heart failure requiring intravenous inotropes, 2nd or 3rd degree AV block (without pacemaker), severe bradycardia, sick sinus syndrome, uncontrolled heart failure, cardiogenic shock, severe peripheral arterial disease, hypotension, metabolic acidosis, untreated pheochromocytoma, severe asthma or COPD.
โ ๏ธ Precautions & Warnings
11th degree AV block, heart failure (avoid if un-controlled), peripheral arterial circulatory disorders (avoid if severe), Prinzmetals angina, myasthenia gravis, lschaemicheart disease, withdraw gradually, history of bronchospasm,diabetes, hyperthyroidis
๐ Drug Interactions
Ca++ antagonists. Antihypertensives including centrally acting agent (e.g. clonidine), antiarrhythmics, antipsychotics.TCADs, MAOls, fluvoxamine, barbiturates, cardiac glycosides, sympathomimetics, cimetidine, hydralazine, rifampicin, insulin/oral hypoglycaemics, NSAIDs, ergot derivatives, erythromycin, anaesthetics, diuretics
โ ๏ธ Adverse Reactions / Side Effects
Cardiovascular effects including bradycardia, postural hypotension, depression, oedema, increased AV block, cardiac arrhythmias, Raynauds phenomenon, cold extremities, sexual dysfunction, GI upset, sleep and CNS disturbances, skin reactions, fatigue, paraesthesia, peripheral neuropathy, arthralgia, myopathy, altered blood sugar haematology and lipid levels. Withdraw if unexplained dry eyes or rash. Rarely, heart failure, dyspnea, bronchospasm
๐คฐ Pregnancy & Lactation Safety
Pregnancy Risk:
Avoid, risk cannot be ruled out.
Lactation / Breastfeeding:
Caution advised or effect undetermined,
๐งช Compatibility & Storage Stability
Compatibility: Stable in NS, D5W, 1/2 NS, LR.
Stability & Storage: Store at approximately 25C (77F). Protect from light, freezing and excessive heat. Discard unused portion. Retain in carton until time of use.
๐ Official Regulatory & Clinical References
- Drug Regulatory Authority of Pakistan (DRAP): Drug Registration, S.R.O. Price Gazettes & National Essential Medicines List (NEML).
- World Health Organization (WHO): Collaborating Centre for Drug Statistics Methodology (ATC/DDD Index).
- Formulary Standards: British National Formulary (BNF) & Pakistan National Formulary (PNF) guidelines.