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CNS stimulants
| Question | Answer |
|---|---|
| What is an Analeptic? | Agents which remove or decrease inhibition from CNS neurons, increase synaptic excitation or alter axonal membrane properties. Net result is CNS stimulation |
| strychnine MOA? | a natural alkaloid which is a disinhibiting analeptic that blocks glycine-mediated postsynaptic inhibition. It is a MOTOR stimulant |
| What are the characteristics of strychnine poisoning? | Tightness of neck and jaw muscles; Hyperreflexia; Tonic extensor thrusts; Tetanic symmetrical; convulsions (opisthotonus); Respiratory arrest |
| How to you treat strychnine poisoning? | IV diazepam, lorazepam, or anesthetic dose of short acting barbiturate; Respiratory support; Quiet surroundings (d/t hyperreflexia may cause seizures); Gastric lavage (only AFTER seizures or risks of seizures have been controlled) |
| Caffiene MOA? | is a xanthine (natural alkaloid) that act as antagonists at adenosine receptors. Adenosine receptors are located on presynaptic terminals of noradrenergic neurons and blocks NE release. So caffeine increases NE release. It is a PSYCHOLOGICAL stimulant |
| What are ADRs of ingesting 1gm caffiene (the equivalent of 12 cups coffee)? | Insomnia, excitement, mild delirium, sensory disturbances; Increased heart rate; Increased respiration |
| What are some other ADRS of caffiene? | it is teratogenic and can cause spontaneous abortions, Tolerance and physical dependence can occur with withdrawal symptoms including lethargy, irritability, and headache |
| Name some amphetamine-type stimulants? | Methylphenidate (Ritalin), Pemoline (Cylert); Phentermine (Fastin); Sibutramine (Meridia); D-amphetamine (Dexedrine); Mixed amphetamine salts (Adderall, Adderall XR); Methamphetamine (Desoxyn); Dexmethylphenidate (Focalin) |
| Amphetamine MOA? | release NE, 5HT, and dopamine from nerve terminals |
| How does Sibutramine (Meridia) differ from other amphetamines? | Sibutramine inhibits reuptake (versus stimulate release) of NE, 5HT, and dopamine |
| Amphetamine ADRs? | Peripheral sympathomimetic effects (e.g., increased blood pressure, stressed CV system); CNS irritability → depression; Abuse potential; Concern about long-term safety of stimulant treatment in children |
| How are amphetamines used? | Nacrolepsy; ADHD |
| Why is pemoline (Cylert) no longer recommended in ADHD treatment? | risk of hepatotoxicity |
| Name 2 amphetamines used for appetite suppression? | phentermine (Adipex-P, Fastin) and sibutramine (Meridia) |
| What class of controlled substance is cocaine? | Class II |
| What is cocaine used for medically? | local anesthetic with vasoconstrictive properties often used in ENT surgeries |
| How does cocaine produce it's CNS effects? | blocks catecholamine (primarily dopamine) reuptake acting on the centers for alertness and responsiveness AND the brain's reward center |
| What are the psychological & physical effects of cocaine? | Produces euphoria (mainly due to dopamine effects), motor restlessness, gradiosity, hypervigilance (due to excessive NE) |
| What is modafinil (Provigil)? | it is NOT an amphetamine but it is a stimulant used in narcolepsy and in people who have problems with day-time sleepiness d/t sleep apnea, shift work, etc.. |
| Modafinil MOA? | Stimulate cells in sleep/wake centers which release the neurotransmitters hypocretin 1 and 2. Results in increased wakefulness |
| Drug interactions with modafinil? | Induces (or increases) CYP3A4 (decreased efficacy of cyclosporine) and inhibits (decreases) CYP2C19 (increased level of clopramine) & CYP2C9 (increased level of warfarin) |
| Name a non-stimulant drug used to treat ADHD? | atomoxetine (Strattera) |
| Atomoxetine MOA? | Selectively inhibits NE transporter, blocking NE reuptake and resulting in increased attention and decreased impulsivity and hyperactivity. Since it doesn’t block DA reuptake, it’s not likely to be abused |
| Ephedra ADRs? | have been associated with heart attacks, sudden cardiac death, stroke, brain hemorrhage, seizures, and deaths |
| What are the subjective effects of LSD? | Heightened awareness of sensory input; synesthesia; Passive observer state; Inward attention; Diminished ability to determine boundaries |
| LSD MOA? | a potent CNS stimulant which may act as an agonist at presynaptic serotonin receptors (5HT1a and 5HT1c) in the midbrain |
| Marijuana MOA? | Bind to specific cannabinoid (CB) receptors located in various brain areas. Endogenous ligands (endocannabinoids) have also been identified. Stimulation of CB receptors leads to activation of brain’s reward center and also activates "eating" centers |
| What is 3,4 methylenedioxymethamphetamine? | MDMA or "Ecstacy" |
| What are the potential ADRs of Ecstacy use? | most significant short-term risk associated with MDMA is impairment of the body’s ability to regulate temperature, resulting in overheating and dehydration. Also causes involuntary grinding of the teeth |
Created by:
psfisher50
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