Drugs Flashcards
Chlorpromazine
Typical [high D2/low 5HT2A block], low potency antipsychotic agent. Good for positive symptoms.
Low potency = less EPSE; more muscarinic, histamine, alpha1 side effects
Haloperidol
Typical [high D2/low 5HT2A block], high potency antipsychotic agent. Good for positive symptoms.
High potency = more EPSE compared to muscarinic, histamine, alpha1 side effects
Clozapine
Atypical [low D2/high 5HT2A block] antipsychotic agent. Mostly used when Pts refractory to other drugs; good for positive and negative symptoms.
ADR: monitor WBC for agranulocytosis; monitor weight gain and increased lipids
Quetiapine
Atypical [low D2/high 5HT2A block] antipsychotic agent.
Fluoxetine
SSRI blocking 5HT reuptake; antidepressant
Less/no sedative/anti-muscarinic action
Side effects include weight gain, sexual dysfunction, and cognitive blunting
Paroxetine
SSRI blocking 5HT reuptake; antidepressant
Less/no sedative/anti-muscarinic action
Side effects include weight gain, sexual dysfunction, and cognitive blunting
Escitralopram
SSRI blocking 5HT reuptake; antidepressant
Less/no sedative/anti-muscarinic action
Side effects include weight gain, sexual dysfunction, and cognitive blunting
Buproprion
NDRI blocking DA and NE reuptake; antidepressant but mostly used in smoking cessation.
Can give anxious, “jacked up” feeling.
Potential for seizures at high doses
Venlafaxine
SNRI: block reuptake of both 5HT and NE, leading to more of the NTs in the synapse.
No sedative/anti-muscarinic action.
Must monitor BP/anxiety.
Trazodone
Mixed 5HT reuptake/partial antagonist/partial agonist
ADR: Sedative effects; postural hypotension.
Mostly used to tx depressed Pts with insomnia
Amitriptyline
TCAD: block reuptake of 5HT and NE, leading to more of the NTs in the synapse.
ADRs: postural hypotension, sedative and anti-muscarinic action.
Can see seizures in OD; OD can be fatal
Phenelzine
MAOI: inhibit degradation of monoamines in the synaptic terminal, resulting in more uptake into vesicle and more vesicular release.
Side effects include postural hypotension and can see seizures, shock, and hyperthermia in OD.
Must be careful of tyramine reaction [hypertensive crisis] when consumed with beer/wine/cheese
Risk of serotonin syndrome when combined with SSRI
Lithium
Use dependent antimanic agent with slow onset [10-21 days].
Mechanism: interferes with Gq cycling [enhance 5HT while diminishing NE/DA].
Side effects include hypothyroidism [anti-TSH], polyuria/polydipsia [anti-ADH].
Competes with Na+ for absorption [increase dietary Na+ = decrease Li+].
Narrow therapeutic index; diuretics can decrease clearance. Can cross BBB and placenta [teratogenic].
Moderate toxicity = confusion, sedation, lethargy, twitching
Severe toxicity = seizures, stupor, coma
Alprazolam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Rapid oral absorption with short half-life [metabolized to active metabolite and then conjugated/inactivated].
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Flurazepam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Long half-life and active metabolite; use can lead to daytime drowsiness [sedative/anxiolytic/hypnotic].
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Diazepam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Rapid oral absorption.
Used to tx broad spectrum epilepsy, status epilepticus in addition to anxiolytic/sedative/hypnotic features.
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Oxazepam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Slow oral absorption. Metabolized directly into inactive metabolite [shorter half-life; better to tx elderly Pts with liver problems]
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Triazolam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present
Rapid oral absorption; metabolized to active metabolite and then conjugated/inactivated [short half-life]. Makes it available as sleep aid as decreases sleep latency with less hangover, but have possibility of rebound insomnia.
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Lorazepam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present
Good IM absorption. Metabolized directly into inactive metabolites [shorter half-lives; the old livers]
Used to tx status epilepticus in addition to anxiolytic/sedative/hypnotic effects
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Midazolam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Used to tx status epilepticus in addition to sedative/hypnotic/anxiolytic features.
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Temazepam
Benzodiazepine: CNS depressant; works to potentiate GABA effects by increasing frequency of Cl- channel opening. Only works with GABA present.
Slow oral absorption. Metabolized to inactive metabolite [short half-life; the old livers].
Greater safety margin as cannot induce general anesthesia at higher doses [no glu activity]; possibility of anterograde amnesia at higher dosages.
Minor withdrawal symptoms but have abuse potential
Flumazenil
Benzodiazepine antagonist used to tx acute benzodiazepine toxicity
Zolpidem
Z-drug: selectively binds alpha1 GABA at benzodiazepine site, leading to sedation without other effects.
Rapid oral absorption, short duration of action, short half-life.
Tx insomnia
Zaleplon
selectively binds alpha1 GABA at benzodiazepine site, leading to sedation without other effects.
Rapid oral absorption, short duration of action, short half-life.
Tx insomnia
