Varenicline

Drug #2195

Varenicline is a partial agonist selective for a4ß2 nicotinic acetylcholine receptor. Varenicline, as the tartrate salt, is a powder which is a white to off-white to slightly yellow solid with the following chemical name: 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino[2,3-h][3]benzazepine, (2R,3R)-2,3-dihydroxybutanedioate (1:1).

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Primary Characteristics

Molecular Weight: 361.35 · Solubility in Water: highly · Non-proprietary name: Varenicline.

Pharmacokinetics

Absorption: Varenicline has an pre-systemic (first-pass) metabolism accounts for 10%.

Distribution: Varenicline has a plasma protein binding is <20%.

Elimination: plasma half-life is 24 hours, renal excretion is 81-92%.

Indications

Varenicline is primarily indicated in conditions like Smoking cessation.

Contraindications

None recorded.

Dosage

Varenicline's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.5 mg	0.5 mg	Every 24h	PO	Day 1-3, Once daily. The patient should set a date to stop smoking. Varenicline dosing should start one week before this date. It should be taken after eating and with a full glass of water. Smoking cessation therapies are more likely to succeed for patients who are motivated to stop smoking and who are provided additional advice and support. Patients should be provided with appropriate educational materials and counseling to support the quit attempt.
0.5 mg	0.5 mg	Every 12h	PO	Day 4-7.
1 mg	1 mg	Every 12h	PO	on day 8, end of treatment.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Varenicline is known to cause more or less tolerable side effects which are usually transient. These include Abnormal dreams, Headache, Insomnia, Nausea.

Warnings / Precautions

Patients who can not tolerate adverse effects of Varenicline may have the dose lowered temporarily or permanently. Patients should be treated with Varenicline for 12 weeks. For patients who have successfully stopped smoking at the end of 12 weeks, an additional course of 12 weeks treatment with Varenicline is recommended to further increase the likelihood of long-term abstinence. Patients who do not succeed in stopping smoking during 12 weeks of initial therapy, or who relapse after treatment, should be encouraged to make another attempt once factors contributing to the failed attempt have been identified and addressed.

Available Brands

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Single Ingredient

Tabs

0.5 mg 1 mg

Storage Conditions

Varenicline should be stored Tabs.

Drug Classification

1.24.7 — Smoking cessation

Manufacturers

Manufacturers of Varenicline in Pakistan:

Pfizer