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Side Effects & Adverse Reactions
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 INVERSINE1 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 When INVERSINE1 is withdrawn, this should be done gradually and other antihypertensive therapy usually must be substituted. On the other hand, the effects of INVERSINE1 sometimes may last from hours to days after therapy is discontinued.
Legal Issues
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Manufacturer Warnings
There is currently no manufacturer warning information available for this drug.
FDA Labeling Changes
There are currently no FDA labeling changes available for this drug.
Uses
For the management of moderately severe to severe essential hypertension and in uncomplicated cases of malignant hypertension.
History
There is currently no drug history available for this drug.
Other Information
INVERSINE®1 (Mecamylamine HCl) is a potent, oral antihypertension agent and ganglion blocker, and is a secondary amine. It is N,2,3,3-tetramethyl-bicyclo [2.2.1] heptan- 2 -amine hydrochloride. Its empirical formula is C11H21N • HCl and its structural formula is:
It is a white, odorless, or practically odorless, crystalline powder, is highly stable, soluble in water and has a molecular weight of 203.75.
INVERSINE1 is supplied as tablets for oral use, each containing 2.5 mg mecamylamine HCl. Inactive ingredients are acacia, calcium phosphate, D&C Yellow 10, FD&C Yellow 6, lactose, magnesium stearate, starch, and talc.
Sources
Inversine Manufacturers
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Targacept, Inc.
Inversine | Targacept, Inc.
Therapy is usually started with one 2.5 mg tablet of INVERSINE1 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 INVERSINE1 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 INVERSINE1.
Administration of INVERSINE1 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.
The effective maintenance dosage should be regulated by blood pressure readings in the erect position and by limitation of dosage to that which causes slight faintness or dizziness in this position. If the patient or a relative can use a sphygmomanometer, instructions may be given to reduce or omit a dose if readings fall below a designated level or if faintness or lightheadedness occurs. However, no change should be instituted without the knowledge of the physician.
Close supervision and education of the patient, as well as critical adjustment of dosage, are essential to successful therapy.
Other Antihypertensive Agents
When INVERSINE1 is given with other antihypertensive drugs, the dosage of these other agents, as well as that of INVERSINE1, should be reduced to avoid excessive hypotension. However, thiazides should be continued in their usual dosage, while that of INVERSINE1 is decreased by at least 50 percent.
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