psychopharm 2 Flashcards
monovalent cation, blocks manic behavior, no behavioral effects in “normals”
Inhibits recycling of inositol substrates, may cause depletion of the 2nd messenger source of PIP2 and therefore reduce the release of IP3 and DAG
lithium
Levels raised by diuretics (Na levels affect excretion and retention), ACE inhibitors, Ang II receptor blockers
lithium side effects
fatigue, tremor, GI symptoms, ataxia higher levels cause hyperactive deep reflexes, rigidity, coma
CI of lithium
pregnancy
clinical uses of lithium
mania, prevent recurrences of bipolar disease, cluster headaches
alternatives to lithium
carbamazepine, valproic acid (Divalproex) for initial control of manic symptoms: haloperidol
Mechanism of action of Antiseizure agents
Alters ion conductance, use dependent effect on Na+ channels; inhibits generation of repetitive action potentials
blocks sodium channels, no interaction with GABA unpredictable absorption, hepatic enzyme induction used for partial seizures, bipolar I disorder and acute manic/mixed episodes
carbamazepine
blocks repetitive neuronal firing, can reduce some Ca currents, increases GABA concentrations; bound to plasma protein, distributes in extracellular fluid used as first line drug in bipolar disease, sedating
valproic acid (Divalproex); inhibits metabolism of drugs including carbamazepine
treatment of depressive episodes associated with bipolar disease (drug combination)
olanzapine and fluoxetine
carbamazepine side effects
CNS side effects such as sedation, confusion and ataxia, diplopia; Teratogen –> Spina Bifida
valproic acid side effects
GI upset, weight gain, hair loss not dose related: hepatotoxicity and teratogenic (spinal bifida)
somatic correlates of anxiety
ANS arousal, voluntary muscle activation (jitteriness, tremor) complications: substance abuse
treatment of anxiety and insomnia
benzodiazepines, SSRIs, buspirone, classical antihistamines, EtOH, cannabis, opiates, barbiturates
benzodiazepine receptor agonists
diazepam, zolpidem
benzodiazepine receptor antagonists
flumazenil
partial agonist for 5-HT 1A, also binds to dopamine receptors delayed onset, little sedation, no dependence or cross-tolerance used for GAS
buspirone
benzodiazepines used to treat anxiety
diazepam, alprazolam, lorazepam
Effects of benzodiazepines
decreased anxiety, sedation, hypnosis, muscle relaxation (diazepam), anterograde amnesia, anticonvulsant action, minimal CV/resp actions alone
benzodiazepine drug interactions
produce additive CNS depression with other depressants; can affect hepatic metabolism of drugs like cimetidine
clinical uses of benzodiazepines
anxiety states, sleep disorders, seizure treatment, IV sedation and anesthesia some used for alcohol withdrawal, acute manic episodes
Antianxiety, rapid onset of action, long duration used as hypnotic
flurazepam
Antianxiety benzodiazepine; Does not form active metabolite; less lipophilic, slower absorption and onset of action, longer duration of action after single dose used as hypnotic
Lorazepam
fast onset of action, high lipid solubility, rapid redistribution; muscle relaxant due to actions in spinal cord; intravenous sedation and anethesia
diazepam
Antianxiety benzo, used for panic disorder
Alprazolam
benzo used for alcohol withdrawl
chlordiazepoxide
symptoms of benzo withdrawal
anxiety, insomnia, irritability, headache, hyperacusis, hallucinations, seizures
Anti-anxiety; high affinity for 5-HT1A receptors, partial agonist; elimination half life: 2-11 hrs; less sedating than benzodiazepines; used for treatment of GAD
Buspirone
other treatments for anxiety
SSRIs & SNRIs, beta-blockers, other sedatives (rarely)
hypnotic that binds to BDZ receptor on GABA complex; weak anxiolytic, muscle relaxant and anticonvulsant; preserves stage 3 and 4 sleep, duration 5-6hr
zolpidem
adverse effects of hypnotic effects
daytime sedation, ataxia, rebound insomnia, tolerance and dependence, occasional idiosyncratic excitement and stimulation
act at GABA A, rapidly absorbed and distributed, highly lipid soluble, renal excretion, additive with other CNS depressants used as anticonvulsant
barbiturate
barbiturate side effects
general CNS depression, anticonvulsant, respiratory depression tolerance (not uniform) physical dependence with withdrawal symptoms (seizures)
skeletal muscle relaxants
used to reduce muscle tone associated with spasticity related to MS injuries/other musculoskeletal disorders
Barbituate hypnotic, anticonvulsant; rarely used today
Phenobarbital
Aldehyde hydrate with pungent taste and somewhat caustic taste; metabolized o tricholoroethanol which is the active form of the drug; Pharmacology similar to barbiturates; Less effects on stages of sleep than benzos and barbiturates
Chloral Hydrate
Muscle relaxant; GABA-mimetic agent working at GABA B receptors, Results in hyperpolarization, causing presynaptic inhibition; decreased release of excitatory transmitters such as glutamate
Baclofen
alpha2 adrenergic agonist, relieves muscle spasm side effects include drowsiness, hypotension, dry mouth interacts with CYP1A2 inhibitors
Tizanidine
other agents used as muscle relaxants
botulinum toxin, dantrolene
