brands

Class

• Beta Blocker

Nigrain commonly prescribed for

(Bold for FDA approved)

How Nigrain works

• For migraine, proposed mechanisms include inhibition of the adrenergic pathway, interaction with the serotonin system and receptors, inhibition of nitric oxide synthesis, and normalization of contingent negative variation

• For tremor, antagonism of peripheral beta 2 receptors is the proposed mechanism

• For PTSD, blockade of beta 1 adrenergic receptors may theoretically prevent fear conditioning and reconsolidation of fear

• For violence/aggression, the mechanism is poorly established; presumed to be related to central actions at beta adrenergic and serotonin receptors

How long until Nigrain works

• For migraine, can begin to work within 2 weeks, but may take up to 3 months on a stable dose to see full effect

• For tremor, can begin to work within days

Notable Side Effects

• Bradycardia, hypotension, hyper- or hypoglycemia, weight gain

• Bronchospasm, cold/flu symptoms, sinusitis, pneumonias

• Dizziness, vertigo, fatigue/tiredness, depression, sleep disturbances

• Sexual dysfunction, decreased libido, dysuria, urinary retention, joint pain

• Exacerbation of symptoms in peripheral vascular disease and Raynaud’s syndrome

Life Threatening Side Effects

• In acute congestive heart failure, may further depress myocardial contractility

• Can blunt premonitory symptoms of hypoglycemia in diabetes and mask clinical signs of hyperthyroidism

• Nonselective beta blockers such as propranolol can inhibit bronchodilation, making them contraindicated in asthma, severe COPD

• Do not use in pheochromocytoma unless alpha blockers are already being used

• Risk of excessive myocardial depression in general anesthesia

weight gain

common

sedation

common

What to do about Nigrain side effects

• Lower dose, change to an extended-release formulation, or switch to another agent

usual dosage range

• 40–400 mg/day

Dosage Forms

• Tablet 10 mg, 20 mg, 40 mg, 60 mg, 80 mg, 90 mg

• Extended-release capsule 60 mg, 80 mg, 120 mg, 160 mg

• Oral solution 4 mg/mL, 8 mg/mL

• Injection 1 mg/mL

long term use

• Safe

habit forming

• No

Renal Impairment

• No dose adjustment necessary

Hepatic Impairment

• Use with caution with severe impairment; dose reduction may be necessary

Cardiac Impairment

• Do not use in acute shock, myocardial infarction, hypotension, and greater than first-degree heart block, but indicated in clinically stable patients post-myocardial infarction to reduce risk of re-infarction starting 1–4 weeks after event

Elderly

• Use with caution

• May increase risk of stroke

Children and Adolescents

• Usual dose in children is 2–4 mg/kg in 2 divided doses; maximum 16 mg/kg/day

• Clinical trials for migraine prophylaxis did not include children

Pregnancy

• Controlled studies have not been conducted in pregnant women

• May reduce perfusion of the placenta

• Use only if potential benefits outweigh the potential risks to the fetus

Breast Feeding

• Some drug is found in mother’s breast milk

• Due to high lipid solubility, propranolol is found in breast milk more than many other beta blockers

• Recommended either to discontinue drug or bottle feed unless the potential benefit to the mother justifies the potential risk to the child