CNS Stimulants

Cocaine MOA

Blocks reuptake of NE, DA, and serotonin (NET, DAT, SERT); also blocks voltage‑gated Na+ channels(local anesthetic) and cardiac K+ channels(pro arrhythmic)

Main CNS effect of cocaine

Increased DA in synapse → euphoria, reward.

Main CV effect of cocaine

Increased NE → tachycardia, hypertension, vasoconstriction. Inc risk of Intracranial hemmorhage, stroke, MI, seizures

Cocaine pharmacologic effects

Increased HR/BP, alertness, euphoria, decreased appetite/sleep, risk of stroke/MI/seizures.

Cocaine overdose risks

Hyperthermia, seizures, coma, death.

Cocaine withdrawal

Depression, dysphoria, bradycardia, anxiety, craving, fatigue, hypersomnolence.

Amphetamine MOA

Substrate for NET/DAT/SERT(blocks reuptake); reverses transporters; inhibits VMAT → increased cytoplasmic monoamines → non‑vesicular DA/NE release.

Most important amphetamine MOA

VMAT inhibition → increased cytoplasmic DA.

Amphetamine effects

Increased wakefulness, alertness, euphoria, decreased appetite; high doses → tachycardia, arrhythmias, stroke.

Amphetamine withdrawal

Dysphoria, drowsiness, irritability.

Common amphetamine products

Dextroamphetamine(Dexedrine), Dextroamphetamine/Amphetamine (Adderall), Lisdexamfetamine (Vyvanse), methamphetamine.

Methylphenidate MOA

Blocks reuptake of NE and DA (NET > DAT >> SERT).

Methylphenidate uses

ADHD.

Stimulant common ADEs

Headache, dizziness, reduced appetite, weight loss, insomnia, irritability, increased BP/HR, tics.

Stimulant rare serious ADEs

Priapism, seizures, stroke, MI, sudden cardiac death, mania, hallucinations.

Long‑term stimulant risks

Mild growth suppression, hypertension/tachycardia, rare sudden cardiac death.

MDMA (Ecstasy) MOA

Reverses monoamine reuptake transporters; serotonin >>> NE, DA.

MDMA effects

Intimacy/empathy, sensory distortion, sexual enhancement.

Two lethal MDMA complications

Hyperthermia and hyponatremia(seizures).

Other MDMA risks

Serotonin syndrome, seizures, dehydration; possible long‑term neurotoxicity.

Phencyclidine (PCP) MOA

NMDA receptor antagonist; inhibits DA/NE/5‑HT reuptake; stimulates sigma receptors.

PCP effects

Hallucinations, agitation, psychosis‑like behavior; sometimes severe sedation; increased BP/HR.

PCP chronic effects

Long‑lasting psychosis even after drug wears off.

Atomoxetine(Strattera) MOA and use

Selective NE reuptake inhibitor. Non stimulant for ADHD, less abuse potential but less effective

Guanfacine MOA, Use, ADEs

Central alpha‑2 agonist. ADHD (extended‑release). ADE: Orthostatic hypotension, fatigue, headache, somnolence, abdominal pain, dry mouth.

Modafinil use, tie?

Narcolepsy + CNS stimulant. Less euphoric and lower abuse potential than amphetamines.

Oxybate salts use + note

Narcolepsy with cataplexy. GHB is oxybate salts in salt form»dangerous

Caffeine class + MOA

Methylxanthine. MOA: Blocks adenosine receptors; inhibits phosphodiesterase → ↑ cAMP/cGMP.

Caffeine Pharmacokinetics

Well absorbed; half‑life ~5 hrs; hepatic metabolism.

Caffeine effects

Increased alertness, mild BP increase, diuresis, headache relief (adjunct), anxiety/insomnia at high doses.

Caffeine medical uses

Apnea of prematurity; adjunct for headaches; wakefulness.

Medical uses of Amphetamines

ADHD, Nacrolepsym Binge eating disorder (Vyvanse)

Step 1 stimulant clues

Sweating, tachycardia, hypertension, hyperactivity → stimulant intoxication; withdrawal → hypersomnolence, irritability, depression.

Step 1 MDMA clue

Party/dancing → hyperthermia + hyponatremia.