Endep Indication:

For the treatment of anxiety, bipolar disorders, and depression.

Endep Mechanism Of Action:

Endep is metabolized to nortriptyline which inhibits the reuptake of norepinephrine and serotonin almost equally. Endep inhibits the membrane pump mechanism responsible for uptake of norepinephrine and serotonin in adrenergic and serotonergic neurons. Pharmacologically this action may potentiate or prolong neuronal activity since reuptake of these biogenic amines is important physiologically in terminating transmitting activity. This interference with the reuptake of norepinephrine and/or serotonin is believed by some to underlie the antidepressant activity of amitriptyline.

Endep Drug Interactions:

Altretamine Risk of severe hypotension
Atazanavir Atazanavir increases the effect and toxicity of tricyclics
Carbamazepine The tricyclics increases the effect of carbamazepine
Cimetidine Cimetidine increases the effect of tricyclic agent
Cisapride Increased risk of cardiotoxicity and arrhythmias
Grepafloxacin Increased risk of cardiotoxicity and arrhythmias
Clonidine The tricyclic decreases the effect of clonidine
Dihydroquinidine barbiturate Quinidine increases the effect of tricyclic agent
Dobutamine The tricyclic increases the sympathomimetic effect
Donepezil Possible antagonism of action
Dopamine The tricyclic increases the sympathomimetic effect
Duloxetine Possible increase in the levels of this agent when used with duloxetine
Epinephrine The tricyclic increases the sympathomimetic effect
Fenoterol The tricyclic increases the sympathomimetic effect
Fluconazole The imidazole increases the effect and toxicity of the tricyclic
Fluoxetine Fluoxetine increases the effect and toxicity of tricyclics
Fluvoxamine Fluvoxamine increases the effect and toxicity of tricyclics
Galantamine Possible antagonism of action
Guanethidine The tricyclic decreases the effect of guanethidine
Isocarboxazid Possibility of severe adverse effects
Isoproterenol The tricyclic increases the sympathomimetic effect
Ketoconazole The imidazole increases the effect and toxicity of the tricyclic
Metaraminol The tricyclic increases the sympathomimetic effect
Mesoridazine Increased risk of cardiotoxicity and arrhythmias
Methoxamine The tricyclic increases the sympathomimetic effect
Moclobemide Possible severe adverse reaction with this combination
Norepinephrine The tricyclic increases the sympathomimetic effect
Orciprenaline The tricyclic increases the sympathomimetic effect
Phenelzine Possibility of severe adverse effects
Phenylephrine The tricyclic increases the sympathomimetic effect
Phenylpropanolamine The tricyclic increases the sympathomimetic effect
Pirbuterol The tricyclic increases the sympathomimetic effect
Pseudoephedrine The tricyclic increases the sympathomimetic effect
Quinidine Quinidine increases the effect of tricyclic agent
Quinidine barbiturate Quinidine increases the effect of tricyclic agent
Rifabutin The rifamycin decreases the effect of tricyclics
Rifampin The rifamycin decreases the effect of tricyclics
Ritonavir Ritonavir increases the effect and toxicity of tricyclics
Rivastigmine Possible antagonism of action
Sibutramine Increased risk of CNS adverse effects
Sparfloxacin Increased risk of cardiotoxicity and arrhythmias
Terbutaline The tricyclic increases the sympathomimetic effect
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Thioridazine Increased risk of cardiotoxicity and arrhythmias
Tranylcypromine Possibility of severe adverse effects
Ephedra The tricyclic increases the sympathomimetic effect
Ephedrine The tricyclic increases the sympathomimetic effect
Mephentermine The tricyclic increases the sympathomimetic effect
Procaterol The tricyclic increases the sympathomimetic effect
Rasagiline Possibility of severe adverse effects
Salbutamol The tricyclic increases the sympathomimetic effect

Endep Food Interactions:

Avoid alcohol.
Take with food to reduce irritation.
Avoid excessive quantities of coffee or tea (Caffeine).
Avoid St.John's Wort.

Endep Generic Name:

Synonyms:

  • Amitriptyline Hydrochloride
  • Amitriptyline HCL
  • Amitriprolidine
  • Amitriptylin
  • Amitryptiline
  • Amitryptyline
  • Amytriptiline

Drug Type:

Small Molecule; Approved

Absorption:

Rapidly and well absorbed following oral administration (bioavailability is 30-60% due to first pass metabolism).

Toxicity (Overdose):

LD50=350 mg/kg (in mice). Symptoms of overdose include abnormally low blood pressure, confusion, convulsions, dilated pupils and other eye problems, disturbed concentration, drowsiness, hallucinations, impaired heart function, rapid or irregular heartbeat, reduced body temperature, stupor, and unresponsiveness or coma.

Protein Binding:

Very highly protein bound (90% or more) in plasma and tissues

Biotransformation:

Exclusively hepatic, with first pass effect. Amitriptyline is demethylated in the liver to its primary active metabolite, nortriptyline.

Half Life:

10 to 50 hours, with an average of 15 hours

Dosage Forms of Endep:

Tablet Oral

Chemical IUPAC Name:

3-(10,11-dihydro-5H-dibenzo-[a,d]cyclohepten-5-ylidene)-N,N-dimethyl-1-propanamine

Organisms Affected:

Humans and other mammals

Endep to general, pharmacology

General, pharmacology..