Inversine

Mecamylamine is used to treat moderate to severe hypertension (high blood pressure). Because of its many side effects, mecamylamine is not commonly used.

Mecamylamine may also be used for purposes other than those listed in this medication guide.

Use caution when driving, operating machinery, or performing other hazardous activities. Mecamylamine may cause dizziness. If you experience dizziness, avoid these activities.

If you experience dizziness, rise slowly from a sitting or lying position to avoid falling.

Use alcohol cautiously. Alcohol may increase drowsiness and dizziness while you are taking mecamylamine.

Take mecamylamine every day at the same time, usually after meals.

Call your doctor if you experience tremor, abdominal pain, abdominal distention, or diarrhea.

Before taking this medication, tell your doctor if you

• have arteriosclerosis (poor blood flow in the arteries, or "hardening of the arteries") in your heart (coronary) or to the head (cerebral);
• have recently had a heart attack;
• have glaucoma;
• have kidney disease; or
• have difficulty urinating as a result of an enlarged prostate or some other cause.

You may not be able to take mecamylamine, or you may require a lower dose or special monitoring during treatment if you have any of the conditions listed above.

Mecamylamine is in the FDA pregnancy category C. This means that it is not known whether mecamylamine will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant.

It is not known whether mecamylamine passes into breast milk. Do not take mecamylamine without first talking to your doctor if you are breast-feeding a baby.

Take mecamylamine exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass of water.

Take mecamylamine after meals.

Take each dose at the same time every day.

Do not stop taking this medication unless your doctor approves. Not taking your medication could make your condition much worse.

Store mecamylamine at room temperature away from moisture and heat.

Seek emergency medical attention.

Symptoms of a mecamylamine overdose include fainting, dizziness, weakness, confusion, nausea, vomiting, diarrhea, constipation, difficulty urinating, anxiety, dry mouth, large pupils, blurred vision, and an irregular heartbeat.

Take the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication.

INVERSINE® (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 • HCI 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.

INVERSINE (mecamylamine) is supplied as tablets for oral use, each containing 2.5 mg mecamylamine HCI. Inactive ingredients are acacia, calcium phosphate, D&C Yellow 10, FD&C Yellow 6, lactose, magnesium stearate, starch, and talc.

Mecamylamine is used to treat moderate to severe hypertension (high blood pressure). Because of its many side effects, mecamylamine is not commonly used.

Mecamylamine may also be used for purposes other than those listed in this medication guide.

Use caution when driving, operating machinery, or performing other hazardous activities. Mecamylamine may cause dizziness. If you experience dizziness, avoid these activities.

If you experience dizziness, rise slowly from a sitting or lying position to avoid falling.

Use alcohol cautiously. Alcohol may increase drowsiness and dizziness while you are taking mecamylamine.

Take mecamylamine every day at the same time, usually after meals.

Call your doctor if you experience tremor, abdominal pain, abdominal distention, or diarrhea.

Before taking this medication, tell your doctor if you

• have arteriosclerosis (poor blood flow in the arteries, or "hardening of the arteries") in your heart (coronary) or to the head (cerebral);
• have recently had a heart attack;
• have glaucoma;
• have kidney disease; or
• have difficulty urinating as a result of an enlarged prostate or some other cause.

You may not be able to take mecamylamine, or you may require a lower dose or special monitoring during treatment if you have any of the conditions listed above.

Mecamylamine is in the FDA pregnancy category C. This means that it is not known whether mecamylamine will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant.

It is not known whether mecamylamine passes into breast milk. Do not take mecamylamine without first talking to your doctor if you are breast-feeding a baby.

Take mecamylamine exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass of water.

Take mecamylamine after meals.

Take each dose at the same time every day.

Do not stop taking this medication unless your doctor approves. Not taking your medication could make your condition much worse.

Store mecamylamine at room temperature away from moisture and heat.

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.

Mecamylamine reduces blood pressure in both normotensive and hypertensive individuals. It has a gradual onset of action (1/2 to 2 hours) and a longlasting effect (usually 6 to 12 hours or more). A small oral dosage often produces a smooth and predictable reduction of blood pressure. Although this antihypertensive effect is predominantly orthostatic, the supine blood pressure is also significantly reduced.

Pharmacokinetics and Metabolism

Mecamylamine is almost completely absorbed from the gastrointestinal tract, resulting in consistent lowering of blood pressure in most patients with hypertensive cardiovascular disease. Mecamylamine is excreted slowly in the urine in the unchanged form. The rate of its renal elimination is influenced markedly by urinary pH. Alkalinization of the urine reduces, and acidification promotes, renal excretion of mecamylamine.

Mecamylamine crosses the blood-brain and placental barriers.

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.