Drugs that bind on biogenic amine transporters Domina Petric, MD

Cocain Inhaled crack cocain absorbs very fast in the lungs and passes into the brain. In the peripheral nervous system cocain inhibits voltage gated sodium channels and blocks action potential. In the central nervous system cocain blocks dopamine, noradrenaline and serotonine reuptake. Blockage of dopamine transporter (DTA) increases the level of dopamine in the nucleus accumbens.

Cocain Activation of sympathetic nervous system is caused by blockage of noradrenaline transporter which causes acute increase of arterial blood pressure, tachycardia and ventricular arrhythmias. Cocain abusers do not have apetite, they are also hyperactive and sleep less.

Cocain Cocaine abuse increases risk for intracranial hemorrhage, ischemic cerebral stroke, acute myocardial infarction and convulsions. Overdose can cause hyperthermia, coma and death.

Cocain Desire for cocain is very strong. Abstinence syndrome Reverse tolerance: patients become sensitive on small cocain dose. Behavioral approach Cocain Desire for cocain is very strong. Supportive care

Amphetamine Amphetamines are indirect sympatomimetics that cause release of endogenous biogenic amines like dopamine and noradrenaline. They decrease normal vesicular release of biogenic amines and increase non vesicular release. Intravenous application! Severe psychical addiction!

Amphetamine Amphetamine and its derivates cause euphoria, psychotic episodes, hallucinations and hyperthermia. They are neurotoxic (probably affecting NMDA receptors). Amphetamine causes tachycardia, vasoconstriction and hypertensive crisis. Abstinence syndrome includes dysphoria and general irritability.

Ecstasy (MDMA) Ecstasy increases intimacy and emphaty without interfering with intellectual capabilities. Ecstasy increases levels of biogenic amines, especially serotonine. Severe MDMA abusers develop severe cognitive disorders. Acute toxic effects include hyperthermia and dehydration.

Ecstasy (MDMA) MDMA can cause serotoninergic syndrome: mental status alterations, autonomic hyperactivity, neuromuscular alterations and convulsions. Dehydration can lead to excessive water intake which causes hyponatremia and convulsions. Abstinence syndrome: depression, agression and bad mood.

Katzung, Masters, Trevor. Clinical pharmacology.