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Winter Exam #3 - Psychomotor Stimulants
n/a
23
Pharmacology
Graduate
01/30/2010

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Term
amphetamine (Benzedrine, Biphetamine, Adderal)
Definition
used to tx ADHD; has greater effect in CNS
Term
d-amphetamine (Dexedrine, Biphetamine, Adderal)
Definition
used to tx ADHD; racemic mixture that has greater effect in CNS
Term
lisdexamfetamine
Definition
prodrug; moderate rate of conversion to main form limits abuse potential
Term
methamphetamine (Desoxyn, "speed", "crank", "ice")
Definition
has methyl group that makes drug resistant to metabolism by MAO & increases its lipid solubility; produces very intense effects in CNS & is widely abused; crystalline form is smokeable
Term
methylphenidate (Ritalin)
Definition
similar to amphetamines; tx of ADHD in children - paradoxical effect of amphetamine, stimulates areas of brain like locus ceruleus enable child to focus attention
Term
cathinone (Khat, "Kat", "Cat")
Definition
found in leaves of khat plant indigenous to Eastern Africa & Mid East; chewing is common in those regions
Term
ephedrine (MaHuang)
Definition
natural product found in herbal preps; used as sympathomimetic agent in varous OTC pep pills
Term
modafanil (Provigil)
Definition
newer drug approved for tx of narcolepsy
Term
Pharmacologic Effects of Amphetamine & Methamphetamine
Definition
CNS: stimulation - increased levels of arousal & wakefulness, euphoria - well-being & confidence, delay of "Fatigue-Induced" decline in performance, tolerance & dependence, rebound effects (crashing), amphetamine psychosis, suppression of appetite; Peripheral: autonomic - HTN, tachycardia, arrhythmias, mydriasis; metabolic - decreased food intake, malnutrition
Term
Toxicity of Amphetamine & Methamphetamine
Definition
sympathomimetics - CV system (HTN, tachycardia, arrhythmias, sudden death); CNS - excessive stimulation, hostility, aggression, psychotic rxns (amphetamine psychosis), tactile hallucinations (Formication)
Term
Mode of Action of Amphetamine, Methamphetamine
Definition
enhanced release & inhibition of uptake of NE & DA; possible direct stimulation of alpha receptors; decreased levels of DA in reward centers of brain
Term
Uses of Amphetamines
Definition
tx of ADHD, narcolepsy, obesity & weight reduction, stimulants, abuse
Term
Pharmacokinetics of Cocaine
Definition
derived from coca plants to mountains of Peru & Columbia; PK: HCl salt - water soluble, absorbed thru mucous membranes ("snorted"), dissolve for IV use; "Crack" form - inhalation of lipid soluble free base forms via smoking; Metabolized in blood by psuedocholinesterases & by liver; when used in combo with EtOH --> long-acting active metabolite formed --> prolongs drug effects
Term
Pharmacological Effects of Cocaine
Definition
local anesthetic (vasoconstriction); CNS - stimulation, increased arousal, euphoria/dysphoria, increased confidence & social activity, POWERFUL REINFORCER, tolerance & dependnce; Peripheral: autonomic - HTN, tachycardia, arrhythmias, suddend death, mydriasis; Teratogenic effects; Deterioration & perforation of nasal septum due to chronic snorting; lung damage & pulmonary edema from smoking; AIDs, Hepatitis from IV use
Term
Cocaine Withdrawal Syndrome
Definition
lethargy, fatigue, & depression; craving for drug; drowsiness, poor concentration, anhedonia, irritability, hostility
Term
Pharmacologic Effects of Caffeine
Definition
CNS - cortical stimulation; increased mental alertness & improvement in some types of mental fcn; respiratory stimulation; tolerance & dependence; Peripheral: cardiac stimulation, vascular effects - peripheral & renal dilation & cerebral constriction, relaxation of bronchioles, stimulatoin of gastric secretion
Term
caffeine
Definition
naturally occurring compound found in coffee, tea, & cocoa plants; used in variety of beverages & some use medicinally; sometimes used to treat apnea in preterm infants
Term
theophylline
Definition
used in tx of asthma; sometimes used to treat apnea in preterm infants
Term
aminophylline
Definition
used in tx of severe asthma
Term
Methylxanthine Overdose
Definition
excessive CNS stimulation which results in life-threatening seizures; Also, excessive cardiac stimulation, eventual cardiovascular collapse; Tx: symptomatic (anticonvulsants, antiarrhythmics)
Term
Uses of Caffeine & its derivatives
Definition
CNS stimulants (OTC energy formulations); asthma; in combo with NSAIDs for HA remedies; OTC diuretic; respiratory stimulant in preterm infants; in beverages
Term
strychnine
Definition
potent convulsant used as rat poison; ANTAGONIST of GLYCINE RECEPTORs in spinal cord; removes post-synaptic inhibitory influences & leads to development of severe toxic seizures; Tx - symptomatic support + diazepam to control seizures
Term
tetanus toxin
Definition
released by Clostridium tetani during infection; produces generalized tetanus & tonic convulsions; acts by inhibiting RELEASE of GLYCINE from Renshaw cells in spinal cord; Tx: symptomatic support, diazepam for seizure control & appropriate antimicrobial therapy
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