DrugInfoSys

Tacrine (HCl)

Drug #1539

A centrally acting reversible cholinesterase inhibitor, which is used to treat mild to moderate dementia of alzheimer's type. It improves cognitive (the operation of the mind by which we become aware of the objects of thoughts or perception) performance.

Primary Characteristics

It is of Synthetic origin.

Molecular Weight: 252.7 · pKa: 9.9 · Solubility in Water: highly · Solubility in Alcohol: highly · Non-proprietary name: Tacrine (HCl).

Molecular structure of Tacrine (HCl)

Pharmacokinetics

Absorption: Tacrine (HCl) has an oral bioavailability is 47.5% (±47.5%), pre-systemic (first-pass) metabolism accounts for 40% (±40%).

Distribution: Tacrine (HCl) has a volume of distribution is 350 litre. plasma protein binding is 55 %.

Elimination: plasma half-life is 2 - 3 hr, renal excretion is < 1 % unchanged.

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Indications

Tacrine (HCl) is primarily indicated in conditions like Alzheimer's disease, Dementia, Respiratory depression.

Contraindications

Tacrine (HCl) is contraindicated in conditions like Anesthesia, Cardiovascular disease, GI diseases, Pulmonary disease, Hypersensitivity.

Dosage

Tacrine (HCl)'s dosage details are as follows:

DoseSingle DoseFrequencyRouteInstructions
Adult Dosage
10 mg10 mgEvery 6hPOFor 6 weeks.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

Unknown4 interactions
4 interactions
Minor2 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Tacrine (HCl) in overdosage may give rise to further complications which include Transaminase elevation.

The signs and symptoms that are produced after acute overdosage of Tacrine (HCl) are Muscular weakness, Increased salivation, Convulsions , Sweating , Vomiting, Nausea, Bradycardia, Hypotension.

Tacrine (HCl) is known to cause more or less tolerable side effects which are usually transient. These include Abdominal pain, Anorexia , Bradycardia , Change in BP, Constipation , Diarrhea, Dyspepsia , Flatulence, Nausea, Skin RashX, Vomiting .

Warnings / Precautions

It should be used only if clearly needed during pregnancy. It should be used with caution in patients with asthma, seizure disorder, epilapsy, heart disease such as hypertension, bradycardia, recent myocardial infraction, thyroid disorders, intestinal disorders, ulcers, urinary problems, impaired liver function or who have a history of such impairment or if have any allergy especially to bromides. Large dose by mouth should be avoided in condition where there may be increase absorption from the gastrointestinal tract. Serum-alanin aminotransferase concentrations should be monitored in patients receiving cintinuous treatment with tacrine. Monitoring should be carried out every other week for atleast the first first 16 weeks of therapy, followd by monthly for 2 months an dthen every 3 months thereafter. Weekly monitoring is recommended in patients with elevated aminotransferase levels that are greater than twice the upper limit of the normal range. If sign of liver involvment worsen, the dose should be reduced or withdrawn. Tacrine should be taken on an empty stomach to improve absorption. The initial dose is given for a minimum of 6 weeks. Dosage should not be increased during this period because the potential exists for a delay in onset of increased liver enzyme concentration. Serum-alanin aminotransferase concentrations should be monitored regularly and if there is no significant increase doses may be increased.

Interference in Pathology

Tacrine (HCl) may interfere in the diagnosis of Liver Function Test (LFT) , Monitoring of liver enzymes.

Available Brands

None recorded.

Storage Conditions

Tacrine (HCl) should be stored Caps.

Drug Classification

  1. 1.20Muscle relaxants and cholinesterase inhibitors