Tetrahydroaminacrine
Tetrahydroaminacrine Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Tetrahydroaminacrine is a brand name. Its generic name is Tacrine.
Tetrahydroaminacrine Introduction
Tetrahydroaminacrine (brand name Cognex) is a reversible acetylcholinesterase inhibitor and was the first approved medication for the treatment of Alzheimer's disease. It is used to help improve cognitive performance in people with mild to moderate Alzheimer's.
Uses for Tetrahydroaminacrine
Tetrahydroaminacrine is used to improve cognitive function in patients with mild to moderate Alzheimer's disease. It works by delaying the breakdown of acetylcholine, a neurotransmitter important in memory and learning functions in the brain.
Mechanism Of Action
Tetrahydroaminacrine works by inhibiting the enzyme acetylcholinesterase, which breaks down the neurotransmitter acetylcholine. By inhibiting its breakdown by acetylcholinesterase, Tetrahydroaminacrine increases the concentration of acetylcholine in the brain, which improves memory and cognitive functions.
How Long Does It Take To Work?
Tetrahydroaminacrine typically takes 4-6 weeks to reach its full effect. However, individual responses vary and some patients may experience benefits sooner.
Absorption
Tetrahydroaminacrine is absorbed rapidly in the body and has a high oral bioavailability. It is metabolized in the liver and has a serum half-life of about 4 hours.
Route of Elimination
Tetrahydroaminacrine is excreted primarily in the bile. About 10% of the drug is eliminated in the feces.
Dosage and Administration
Tetrahydroaminacrine is available as 10mg, 20mg, and 30mg tablets. The usual dose is 10mg three times a day, 20mg two times a day, or 30mg once a day. It is typically taken with food to reduce gastrointestinal side effects.
Side Effects
The most common side effects of tacrine include gastrointestinal disturbances, such as nausea and vomiting. It can also cause headaches, increased sweating, weight loss, and changes in liver function tests.
Toxicity
Tetrahydroaminacrine can be moderately to severely toxic if taken in large doses. In cases of severe toxicity, death can occur. Symptoms of severe toxicity include vomiting, muscle weakness, shortness of breath, confusion, and seizures.
Precautions
Tetrahydroaminacrine should be used with caution in patients with a history of liver or kidney disease, or in patients taking medications which can affect the liver. Tetrahydroaminacrine can also increase the risk of gastrointestinal bleeding if used in combination with other medications such as non-steroidal anti-inflammatory drugs.
Interactions
Tetrahydroaminacrine can interact with other medications and can increase or decrease the effect of those medications. For example, tacrine can increase the effect of antidepressants, and also has the potential to interact with warfarin, a blood thinner.
Disease Interactions
Tetrahydroaminacrine can worsen certain diseases and should not be used in patients with a history of seizure disorders, asthma, closed angle glaucoma, or intestinal obstruction. It can also interact with other disease states, making them worse.
Drug Interactions
Tetrahydroaminacrine can interact with other medications, including antidepressants, antihistamines, bradycardia medications, anticonvulsants, and anti-anxiety medications. It is important to discuss any medications you are taking with your doctor before starting tacrine therapy.
Food Interactions
Tetrahydroaminacrine can interact with certain foods, such as grapefruit and pomegranate juice. Eating these foods while taking tacrine can increase or decrease its effectiveness.
Pregnancy Use
Tetrahydroaminacrine should not be used during pregnancy, as it can cause harm to an unborn fetus. Women who are pregnant or planning to become pregnant should discuss their use of tacrine with their physician.
Lactation Use
Tetrahydroaminacrine is not recommended for use in women who are breastfeeding.
Acute Overdose
An overdose of Tetrahydroaminacrine can cause severe symptoms, including difficulty breathing, seizures, and even death. If an overdose is suspected, seek immediate medical attention.
Contraindication
Tetrahydroaminacrine should not be used in patients with a known hypersensitivity to the drug or anyone who has a history of seizures or movement disorders. It should also not be used in combinations with certain drugs, such as muscle relaxants.
Use Direction
Tetrahydroaminacrine should be taken as directed by your doctor. It is typically taken with food to reduce gastrointestinal side effects. Patients should not exceed the recommended dose and should not take more than two doses in one day.
Storage Condition
Tetrahydroaminacrine should be stored at room temperature, away from direct light and heat. It should be kept out of reach of children and pets.
Volume Of Distribution
The volume of distribution of tacrine is 6.6 L/kg.
Half Life
The half-life of Tetrahydroaminacrine is 4 hours.
Clearance
The clearance of tacrine is 19 mL/min/kg.
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