Egleton: Anxiolytics Flashcards
(25 cards)
Fluoxetine/ Sertraline: use and side effects
SSRIs
For PTSD and most anxiety disorders
Very slow onset of action (2-4 wks)
Jitters
Venflaxine
SNRIs Similar to SSRI + NE Treat depression Desensitize NE receptor, normalize amygdala activation and CSTC PTSD Slow onset (2-4wk) Jitters
Anti-jitters
Benzodiazepine
Imipramine
TCA Similar to SSRI and SNRI More side effects Second line GAD and Panic disorders Slow onset (2-4wk) Jitters
Benzodiazepine: MoA
Enhance GABA binding to GABA A receptor Increase frequency of channel opening Increaser Cl flux into cell Hyperpolarization Inhibit cell activity
Benzodiazepine: CNS effect
Relief of anxiety
Sleep induction
Anesthetic effects
(Tapers off before Coma and Death)
Benzodiapine: considerations
Don’t give to pregnant/ breastfeeding mother (cross placenta/ secreted in milk/ lipophilic)
Antacid prevent absorption from gut
Benzodiazepine: metabolism
Longer metabolite half life than parent
Hepatic metabolism
Phase I inhibited by Cimetidine
Oxazepam/ Lorazepam
Benzodiazepine
Useful for liver disease patient and elderly
No metabolites
Short half life
Benzodiazepine: side effects
Drowsiness and Confusion
Anterograde amnesia (1-3 hr after dose) for Anesthesia
Rebound
Interact with alcohol and other depressant= Resp. depression/ Coma
Benzodiazepine: contra
COPD: Midazolam= worse with Asthma, Chronic bronchitis, Emphysema
Obstructive sleep apnea: aggravate sleep related breathing disorder
Liver disease: potentiated BDZ effects
Must reduce dose for elderly
Alcohol: overdose with respiratory depression
Pregnancy
Benzodiazepine: tolerance/ dependence
No tolerance to anxiolytic effects (others do)
Physical dependence can occur if extended therapy
Benzodiazepine: withdrawal
More severe for shorter half life
Anxiety, Insomnia
Seizure (rare){for treatment of seizure}
Diazepam: unique property
BDZ
Direct muscle relaxant
Alprazolam: unique property
BDZ
Antidepressant, Panic disorder, Agoraphobia
Trizolam: unique property
BDZ
Rebound anxiety and Rebound insomnia
Lorazepam: unique property
Antiemetic
Flumazenil
BDZ antagonist Antagonist for BDZ overdose IV admin May precipitate withdrawal/ cause seizure with BDZ use for anticonvulsant ADR: dizziness, nausea, vomit, agitation
Buspirone
Non-BDZ Agonist of 5HT1A (post and presynaptic) Treat GAD (generalized anxiety disorder) Lack sedative= for pilots and doctors No interaction with alcohol and other CND depressants Good for elderly with substance abuse
Pregabalin
Blocks Voltage sensitive Ca channels (VSCC)
Binds presynaptic N and P/Q channel
Prevent release of exitatory neurotransmitters in Amygdala/ CTSC
For GAD, Social generalized
Meprobamate
Not as effective as BDZ
For anxiety
Contra: Porphyrias
Propanolol
Nonselective beta-adrenergic blocker
Reduce somatic symptoms of anxiety (palpitation, sweating, tachycardia)
For short term Situational anxiety, stage/ exam fright
Hydroxyzine
Antihistamine (H1 receptor antagonist)
Cause sedation
For GAD + insomnia
Mirtazapine
5HT2 receptor angatonist
For GAD + insomnia
ADR: Weight gain and Sedation