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Mecamylamine: Drug information

Mecamylamine: Drug information
(For additional information see "Mecamylamine: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Vecamyl
Pharmacologic Category
  • Ganglionic Blocking Agent
Dosing: Adult
Hypertension

Hypertension: Oral: Initial: 2.5 mg twice daily; may increase in increments of 2.5 mg/day at intervals ≥2 days until desired BP response is achieved; if divided doses are not the same, give the smaller dose in the morning and larger dose(s) in the afternoon; average dose: 25 mg/day (usually in 3 divided doses, but more frequent dosing may be required). Note: Avoid abrupt discontinuation; gradual tapering is recommended.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling; use with caution; use with extreme caution, if at all, if renal impairment is manifested by a rising or elevated BUN. Use is contraindicated in uremia.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Tablet, Oral, as hydrochloride:

Vecamyl: 2.5 mg

Generic Equivalent Available: US

No

Administration: Adult

Oral: The morning dose should be relatively small and, in some instances, may even be omitted; the larger dose should be given at noon time and possibly in the evening. Administration after meals may cause a more gradual absorption and smoother control of excessively high BP; timing of relationship to meals should be consistent.

Use: Labeled Indications

Hypertension: Management of moderately severe to severe hypertension and in uncomplicated malignant hypertension.

Medication Safety Issues

Sound-alike/look-alike issues:

Mecamylamine may be confused with mesalamine

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.

Cardiovascular: Orthostatic hypotension, syncope

Central nervous system: Altered mental status, choreiform movements, convulsions, fatigue, orthostatic dizziness, paresthesia, sedation

Endocrine & metabolic: Decreased libido

Gastrointestinal: Anorexia, constipation (sometimes preceded by small, frequent stools), glossitis, intestinal obstruction, nausea, vomiting, xerostomia

Genitourinary: Impotence, urinary retention

Neuromuscular & skeletal: Tremor, weakness

Ophthalmic: Blurred vision, mydriasis

Respiratory: Pulmonary edema, pulmonary fibrosis

Contraindications

Hypersensitivity to mecamylamine or any component of the formulation; mild, moderate, labile hypertension (may not be suitable for uncooperative patients); coronary insufficiency or recent myocardial infarction; uremia; glaucoma; organic pyloric stenosis; coadministration with antibiotics or sulfonamides

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: CNS effects, including tremor, choreiform movements, mental aberrations, and convulsions may occur (rarely), especially with large doses or in patients with cerebral or renal insufficiency. In addition, dizziness, lightheadedness, or fainting may also occur.

• Paralytic ileus: Discontinue if signs of paralytic ileus occur (eg, frequent loose bowel movements with abdominal distention, decreased borborygmi)

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with marked cerebral and coronary arteriosclerosis or after a recent cerebral accident.

• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia, bladder obstruction, or urethral stricture; may cause urinary retention.

• Renal impairment: Use with caution in patients with renal impairment. When renal impairment is manifested by a rising or elevated BUN, use with extreme caution, if at all. Since mecamylamine is excreted unchanged in the urine, renal impairment may reduce elimination and increase the risk of adverse effects including hypotension; the risk for neurological adverse effects is increased especially when large doses are administered to patients with renal impairment.

Other warnings/precautions:

• Abrupt discontinuation: Do not abruptly discontinue.

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alcohol (Ethyl): May enhance the adverse/toxic effect of Mecamylamine. Risk C: Monitor therapy

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Alkalinizing Agents: May increase the serum concentration of Mecamylamine. Risk C: Monitor therapy

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When used at chemotherapy doses, hold blood pressure lowering medications for 24 hours before amifostine administration. If blood pressure lowering therapy cannot be held, do not administer amifostine. Use caution with radiotherapy doses of amifostine. Risk D: Consider therapy modification

Aminoglycosides: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Risk C: Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Risk C: Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Risk X: Avoid combination

Capreomycin: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Colistimethate: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Risk C: Monitor therapy

Flunarizine: May enhance the therapeutic effect of Antihypertensive Agents. Risk C: Monitor therapy

Herbal Products with Blood Pressure Increasing Effects: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy

Herbal Products with Blood Pressure Lowering Effects: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Risk C: Monitor therapy

Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Risk C: Monitor therapy

Lincosamide Antibiotics: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Loop Diuretics: May enhance the hypotensive effect of Antihypertensive Agents. Risk C: Monitor therapy

Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Risk C: Monitor therapy

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Risk C: Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Risk D: Consider therapy modification

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Risk C: Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Polymyxin B: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy

Sulfonamides: May enhance the adverse/toxic effect of Mecamylamine. Risk X: Avoid combination

Tetracyclines: May enhance the neuromuscular-blocking effect of Mecamylamine. Risk X: Avoid combination

Thiazide and Thiazide-Like Diuretics: May enhance the adverse/toxic effect of Mecamylamine. Management: Consider avoiding the use of mecamylamine and thiazide diuretics. If combined, mecamylamine prescribing information suggests reducing the mecamylamine dose by 50% in order to avoid excessive hypotension. Risk D: Consider therapy modification

Urinary Acidifying Agents: May decrease the serum concentration of Mecamylamine. Risk C: Monitor therapy

Vasopressin: Mecamylamine may enhance the therapeutic effect of Vasopressin. Specifically, the effect of vasopressin on mean arterial blood pressure may be increased. Risk C: Monitor therapy

Pregnancy Considerations

Mecamylamine crosses the placenta.

Breastfeeding Considerations

Due to the potential for serious adverse reactions in the nursing infant, the manufacturer recommends a decision be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother.

Dietary Considerations

Take after meals. Concomitant use of alcohol may potentiate the effects of mecamylamine.

Monitoring Parameters

Monitor BP (assess in the erect position before initiation and with dose increases), orthostatic vital signs, and heart rate.

Mechanism of Action

Mecamylamine inhibits acetylcholine at the autonomic ganglia, causing a decrease in blood pressure. The blood pressure lowering effect is predominantly orthostatic; the supine blood pressure is also significantly decreased.

Pharmacokinetics

Onset: 0.5 to 2 hours

Duration: 6 to ≥12 hours

Absorption: Almost complete

Excretion: Urine (unchanged); rate of elimination is significantly affected by the pH of the urine. Acidic urine promotes excretion; alkalinization reduces excretion

Pricing: US

Tablets (Vecamyl Oral)

2.5 mg (per each): $75.84

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

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