CNS stimulatnts Flashcards
Amphetamines- MOA
increase the release and inhibit the reuptake of NE and DA
may directly stimulate alpha receptors in the reward centers of the brain.
Chronically decreases levels of DA in reward centers of the brain
Amphetamines- kinetics
Injected, oral, snorted, or smoked
liver metabolism and renal excretion
Enhanced excretion in acidic urine
How do you acidify urine
ASA and Vitamin C
inc excretion before a drug test
Amphetamines- CNS AE
Psychosis- schizophrenia- reversible
aggression and hostility
formication- tactile hallucinations
Amphetamines CV- AE
arrhythmia, sudden death, tachycardia, HTN
Amphetamines metabolic AE
malnutrition secondary to dec food intake
Amphetamine dental or skin AE
constriction of BV in the skin and oral mucosa causing lesions with dec healing esp with formications which cause scratching
Amphetamine rebound
patients may crash from amphetamine use leading to cycles of use
Amphetamine- Tolerance/ Dependence/ withdrawal
Psychological and physical dependence,
withdrawal symptoms of fatigue, lethargy, and depression
Amphetamine- CNS actions
stimulates arousal and wakefulness
euphoria
performance enhancement
appetite suppression
Amphetamine uses
narcolepsy ADHD weight loss- thought not anymore stimulants drug abuse
what NT does the structure of the prototype amphetamine resemble
NE/ Epi
what is Adderral
racemic mixture of salts that dissolve at different rates allowing for a longer duration of action
D-amphetamine
D-isomer of amphetamine which has more powerful CNS effects
Lisdexamfetamine
Prodrug- amphetamine + lysine. This lysine has to be cleaved off in the liver before the drug is activated.
Intended to limit abuse potential, but didn’t work
Methamphetamine
amphetamine with an extra methylgroup which makes it resistant to MAO breakdown –> inc T1/2 and lipid solubility leading to drug abuse
other names include- speed, crank, ice, and meth
Methylphenidate
Ritalin- used to limit hyperactivity of ADHD
stimulates the locus cerruleus to enhance focus
cathinone
Kaht leaves contain this as stimulants
Was sold as bath salts
Ephedrine
stimulates alpha receptors
OTC diet pills that have been banned b/c of their cardiotoxic effects.
Weight loss aids that contained this –> tolerance, abuse, and in the longterm were not effective
Modafanil
Treats narcolepsy
Cocaine MOA
blocks reuptake of DA in the nucleus accumbens (reward center)
Effects of cocaine
Confidence, reinforcement, euphoria
Cocaine- results of chronic use
DA levels in neurons are depleted and the opposite effects occur –>craving, dependence, crash
Cocaine- Kinetics, different forms
Powered HCl salt- water soluble- snort or ingest
Free base, Crack: dehydrated, fat soluble- smoke it
Cocaine AE
teratogenic, addictive, nasal septum deterioration, IV drug use risks CNS CV metabolic dental/skin same AE as stimulants
Treating Cocaine dependence
L-DOPA
Nutritional supplements that inc DA
bromocriptine, buproprion, buprenorphine
