Aminoadamantane

Aminoadamantane Uses, Dosage, Side Effects, Food Interaction and all others data.

The mechanism by which amantadine exerts its antiviral activity is not clearly understood. It appears to mainly prevent the release of infectious viral nucleic acid into the host cell by interfering with the function of the transmembrane domain of the viral M2 protein. In certain cases, amantadine is also known to prevent virus assembly during virus replication. It does not appear to interfere with the immunogenicity of inactivated influenza A virus vaccine.

Aminoadamantane inhibits the replication of influenza A virus isolates from each of the subtypes, i.e., H1N1, H2N2 and H3N2. It has very little or no activity against influenza B virus isolates. A quantitative relationship between the in vitrosusceptibility of influenza A virus to amantadine and the clinical response to therapy has not been established in man. Sensitivity test results, expressed as the concentration of amantadine required to inhibit by 50% the growth of virus (ED50) in tissue culture vary greatly (from 0.1 µg/mL to 25.0 µg/mL) depending upon the assay protocol used, size of virus inoculum, isolates of influenza A virus strains tested, and the cell type used. Host cells in tissue culture readily tolerated amantadine up to a concentration of 100 µg/mL.

Aminoadamantane is an antiviral drug which also acts as an antiparkinson agent, for which it is usually combined with L-DOPA when L-DOPA responses decline (probably due to tolerance). It is a derivate of adamantane, like a similar drug rimantadine. The mechanism of action of amantadine in the treatment of Parkinson's disease and drug-induced extrapyramidal reactions is not known. It has been shown to cause an increase in dopamine release in the animal brain, and does not possess anticholinergic activity.

Trade Name Aminoadamantane
Availability Prescription only
Generic Amantadine
Amantadine Other Names Amantadina, Amantadine, Amantadinum, Amantidine, Aminoadamantane
Related Drugs Sinemet, Rytary, Gocovri, Sinemet CR, diphenhydramine, Benadryl, ropinirole, pramipexole, benztropine, carbidopa / levodopa
Type
Formula C10H17N
Weight Average: 151.2487
Monoisotopic: 151.136099549
Protein binding

Approximately 67% bound to plasma proteins over a concentration range of 0.1 to 2.0 µg/mL.

Groups Approved
Therapeutic Class Respiratory viral infections (Influenza)
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Aminoadamantane
Aminoadamantane

Uses

Aminoadamantane Hydrochloride is used for-

  • Treatment of parkinsonism
  • Treatment of drug-induced extrapyramidal reactions
  • Prophylaxis and treatment of signs and symptoms of infection caused by various strains of influenza A virus

Aminoadamantane is also used to associated treatment for these conditions: Cerebral Arteriosclerosis, Chorea, Extrapyramidal disorder caused by neuroleptic drugs without Tardive dyskinesia, Fatigue, Influenza A Virus Infection, Parkinson's Disease (PD), Parkinsonism, Parkinsonism post encephalitic, Restless Legs Syndrome (RLS)

How Aminoadamantane works

The mechanism of its antiparkinsonic effect is not fully understood, but it appears to be releasing dopamine from the nerve endings of the brain cells, together with stimulation of norepinephrine response. It also has NMDA receptor antagonistic effects. The antiviral mechanism seems to be unrelated. The drug interferes with a viral protein, M2 (an ion channel), which is needed for the viral particle to become "uncoated" once it is taken inside the cell by endocytosis.

Dosage

Aminoadamantane dosage

Parkinson's disease:

  • Adult: Initially, 100 mg/day, increased to 100 mg bid after a wk or more. Max dose: 400 mg daily.
  • Elderly: >65 yr: Lowest effective dose.

Prophylaxis of influenza A:

  • Adult: 100 mg daily for up to 6 wk; when used with influenza vaccination: only up to 3 wk after vaccination.
  • Child: 10-15 yr: 100 mg daily.

Influenza A:

  • Adult: 100 mg daily for 5 days.
  • Elderly: >65 yr: Daily dose of 1 day.

Herpes zoster in immunocompromised patients:

  • Adult: 100 mg bid for 14 days, continued for another 14 days if pain persists.

Side Effects

The adverse effects of Aminoadamantane are generally mild and, when they occur, may diminish or cease after a week or more on the medication. The most commonly reported side effects include nausea, dizziness/ lightheadedness, and insomnia.

Other side effects may include edema of ankles, livedo reticularis; anxiety, elevation of mood, headache, lethargy, hallucinations, ataxia, slurred speech, blurred vision, loss of concentration, nervousness, depression, myalgia, palpitations, orthostatic hypotension, dry mouth, anorexia, constipation and diaphoresis.

Toxicity

Deaths have been reported from overdose with amantadine. The lowest reported acute lethal dose was 2 grams. Drug overdose has resulted in cardiac, respiratory, renal or central nervous system toxicity. Cardiac dysfunction includes arrhythmia, tachycardia and hypertension. Pulmonary edema and respiratory distress (including ARDS) have been reported. Renal dysfunction including increased BUN, decreased creatinine clearance and renal insufficiency can occur. Central nervous system effects that have been reported include insomnia, anxiety, aggressive behavior, hypertonia, hyperkinesia, tremor, confusion, disorientation, depersonalization, fear, delirium, hallucination, psychotic reactions, lethargy, somnolence and coma. Seizures may be exacerbated in patients with prior history of seizure disorders. Hyperthermia has also been observed in cases where a drug overdose has occurred.

Precaution

Aminoadamantane should not be discontinued abruptly in patients with Parkinson's disease since a few patients have experienced a parkinsonian crisis, i.e., a sudden marked clinical deterioration, when this medication was suddenly stopped. The dose of anticholinergic drugs or of Aminoadamantane Hydrochloride should be reduced if atropine-like effects appear when these drugs are used concurrently. Abrupt discontinuation may also precipitate delirium, agitation, delusions, hallucinations, paranoid reaction, stupor, anxiety, depression and slurred speech.

Interaction

Concurrent administration of Aminoadamantane and anticholinergic agents or levodopa may increase confusion, hallucinations, nightmares, gastro-intestinal disturbances, or other atropine-like side effects. Psychotic reactions have been observed in patients receiving Aminoadamantane and Levodopa.

Concurrent administration of Aminoadamantane and drugs or substances (e.g. alcohol) acting on the CNS may result in additive CNS toxicity. Close observation is recommended.

Food Interaction

  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

Volume of Distribution

  • 3 to 8 L/kg [healthy subjects]

Elimination Route

Aminoadamantane is well absorbed orally from the gastrointestinal tract.

Half Life

Mean half-lives ranged from 10 to 14 hours, however renal function impairment causes a severe increase in half life to 7 to 10 days.

Clearance

  • 0.2 - 0.3 L/hr/kg
  • 0.10 +/- 0.04 L/hr/kg [healthy, elderly male]

Elimination Route

It is primarily excreted unchanged in the urine by glomerular filtration and tubular secretion.

Pregnancy & Breastfeeding use

Pregnancy category C. No well-controlled studies have been done in pregnant women to evaluate Aminoadamantane's safety. Aminoadamantane may be used during pregnancy when the potential benefits outweigh the potential but unknown risks to the fetus.

Aminoadamantane is excreted into breast milk in low concentrations. As no information is available on the effects in infants, therefore amantadine should be used cautiously in women who are breastfeeding.

Contraindication

Aminoadamantane is contraindicated in patients with known hypersensitivity to the active substances or to any of the excipients.

Special Warning

Patients with renal impairment: The dose should be reduced. This can be achieved by either reducing the total daily dose, or by increasing the dosage interval in accordance with the creatinine clearance. For example:

  • CrCl <15 ml/min: Contraindicated
  • CrCl 15-35 ml/min: 100 mg every 2 to 3 days
  • CrCl >35 ml/min: 100mg every day

Patients with hepatic impairment: Use with caution

Storage Condition

Store at 20-25°C in dry place. Protect from light.

Innovators Monograph

You find simplified version here Aminoadamantane

Aminoadamantane contains Amantadine see full prescribing information from innovator Aminoadamantane Monograph, Aminoadamantane MSDS, Aminoadamantane FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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