pharmacopeia
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/api/v1/drug/mecamylamine

Mechanism of action

Sourced from openFDA

Mechanism-of-action class: Cholinergic Nicotinic Antagonists.

Cholinergic Nicotinic

Indications

Sourced from openFDA
  • For the management of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension.ICD-10: I10

Contraindications

Sourced from openFDA
  • Mecamylamine HCl should not be used in mild, moderate, labile hypertension and may prove unsuitable in uncooperative patients. It is contraindicated in coronary insufficiency or recent myocardial infarction.contraindicated

Dosage & administration

Sourced from openFDA

Therapy is usually started with one 2.5 mg tablet of Mecamylamine HCl twice a day. This initial dosage should be modified by increments of one 2.5 mg tablet at intervals of not less than 2 days until the desired blood pressure response occurs (the criterion being a dosage just under that which causes signs of mild postural hypotension). The average total daily dosage of Mecamylamine HCl is 25 mg, usually in three divided doses. However, as little as 2.5 mg daily may be sufficient to control hypertension in some patients. A range of two to four or even more doses may be required in severe cases when smooth control is difficult to obtain. In severe or urgent cases, larger increments at smaller intervals may be needed. Partial tolerance may develop in certain patients, requiring an increase in the daily dosage of Mecamylamine HCl. Administration of Mecamylamine HCl after meals may cause a more gradual absorption and smoother control of excessively high blood pressure. The timing of doses in relation to meals should be consistent. Since the blood pressure response to antihypertensive drugs is increased in the early morning, the larger dose should be given at noontime and perhaps in the evening. The morning dose, as a rule, should be relatively small and in some instances may even be omitted. The initial regulation of dosage should be determined by blood pressure readings in the erect position at the time of maximal effect of the drug, as well as by other signs and symptoms of orthostatic hypotension.

Warnings & precautions

Sourced from openFDA

Mecamylamine, a secondary amine, readily penetrates into the brain and thus may produce central nervous system effects. Tremor, choreiform movements, mental aberrations, and convulsions may occur rarely. These have occurred most often when large doses of Mecamylamine HCl were used, especially in patients with cerebral or renal insufficiency. When ganglion blockers or other potent antihypertensive drugs are discontinued suddenly, hypertensive levels return. In patients with malignant hypertension and others, this may occur abruptly and may cause fatal cerebral vascular accidents or acute congestive heart failure. When Mecamylamine HCl is withdrawn, this should be done gradually and other antihypertensive therapy usually must be substituted. On the other hand, the effects of Mecamylamine HCl sometimes may last from hours to days after therapy is discontinued.

Adverse reactions

Sourced from openFDA

The following adverse reactions have been reported and within each category are listed in order of decreasing severity. Gastrointestinal: Ileus, constipation (sometimes preceded by small, frequent liquid stools), vomiting, nausea, anorexia, glossitis and dryness of mouth. Cardiovascular: Orthostatic dizziness and syncope, postural hypotension. Nervous System/Psychiatric: Convulsions, choreiform movements, mental aberrations, tremor, and paresthesias (see WARNINGS ). Respiratory: Interstitial pulmonary edema and fibrosis. Urogenital: Urinary retention, impotence, decreased libido. Special Senses: Blurred vision, dilated pupils. Miscellaneous: Weakness, fatigue, sedation.

Use in specific populations

Sourced from openFDA

Pregnancy Pregnancy Category C. Animal reproduction studies have not been conducted with Mecamylamine HCl. It is not known whether Mecamylamine HCl can cause fetal harm when given to a pregnant woman or can affect reproductive capacity. Mecamylamine HCl should be given to a pregnant woman only if clearly needed.

Pharmacokinetics

Sourced from openFDA
Metabolism
and Metabolism Mecamylamine HCl is almost completely absorbed from the gastrointestinal tract, resulting in consistent lowering of blood pressure in most patients with hypertensive cardiovascular disease. Mecamylamine HCl is excreted slowly in the urine in the unchanged form.

Overdosage

Sourced from openFDA

Signs of overdosage include: hypotension (which may progress to peripheral vascular collapse), postural hypotension, nausea, vomiting, diarrhea, constipation, paralytic ileus, urinary retention, dizziness, anxiety, dry mouth, mydriasis, blurred vision, or palpitations. A rise in intraocular pressure may occur. Pressor amines may be used to counteract excessive hypotension. Since patients being treated with ganglion blockers are more than normally reactive to pressor amines, small doses of the latter are recommended to avoid excessive response. The oral LD 50 of Mecamylamine HCl in the mouse is 92 mg/kg.

Approval history

Sourced from openFDA
  • Mar 19, 2013ANDAANDA204054Lgm Pharma

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
10 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Abdominal Distension220%
  2. 2Constipation220%
  3. 3Dizziness220%
  4. 4Fatigue220%
  5. 5Abdominal Pain110%
  6. 6Abnormal Faeces110%
  7. 7Aggression110%
  8. 8Diarrhoea110%
  9. 9Drug Ineffective110%
  10. 10Drug Level Increased110%
  11. 11Dyskinesia110%
  12. 12Gastrointestinal Bacterial Infection110%
  13. 13Gastrointestinal Disorder110%
  14. 14General Physical Health Deterioration110%
  15. 15Hospitalisation110%

Literature

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Recent PubMed references pinned to Mecamylamine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 31 ClinicalTrials.gov registrations naming Mecamylamine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Mecamylamine work?
Mechanism-of-action class: Cholinergic Nicotinic Antagonists.
What is Mecamylamine used for?
According to FDA labeling, Mecamylamine carries indications including: For the management of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Mecamylamine?
Mecamylamine is classified as Secondary and tertiary amines, Autonomic Ganglionic Blocker, Cholinergic Nicotinic Antagonists, Decreased Autonomic Ganglionic Activity, Decreased Autonomic Nervous System Acetylcholine Activity, Decreased Blood Pressure, Decreased Central Nervous System Acetylcholine Activity.
What are the brand names for Mecamylamine?
Mecamylamine is marketed under brand names including Vecamyl.
What are the contraindications for Mecamylamine?
Mecamylamine labeling lists contraindications including: Mecamylamine HCl should not be used in mild, moderate, labile hypertension and may prove unsuitable in uncooperative patients. It is contraindicated in coronary insufficiency or recent myocardial infarction.. Always consult the full prescribing information and a clinician.
Note. Data for mecamylamine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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