A.23 Flashcards
Benzodiazepines
Diazepam,
Nitrazepam,
Midazolam,
Alprazolam,
Clonazepam,
Flumazenil
Diazepam
MOA: GABAA-R agonist;
Effect: Cl- influx→ hyperpolarization→ muscle relaxant effect;
IND: used in pediatrics, premedication/procedural sedation, Anesthesia, preoperative sedation, muscle spasticity (central acting sk.m.relaxant), anxiety, withdrawal states (e.g.alcohol);
SEs: sedation, amnesia, dependance, tolerance, sleeping patterns are not physiological;
Extra: long acting active metabolite, hepatic metabolism;
Dosage: p.o 5-10mg, status epilepticus i.v. 30mg;
DOA: 60h+active metabolite ~150h;
ROA: p.o, i.v, p.r
Clonazepam
MOA: GABAA-R agonist;
Effect: Cl- influx→ hyperpolarization→ muscle relaxant effect;
IND: anxiety, panic attacks, bipolar disorders, antiepileptic;
SEs: sedation, amnesia, dependance, tolerance, sleeping patterns are not physiological;
Extra: long acting, hepatic metabolism;
DOA: 30h;
ROA: P.O, i.v
Alprazolam
MOA: GABAA-R agonist;
Effect: Cl- influx→ hyperpolarization→ muscle relaxant effect;
IND: Anxiety, panic attacks and phobic disorders;
SEs: sedation, amnesia, dependance, tolerance, sleeping patterns are not physiological;
Extra: intermediate acting, hepatic metabolism;
DOA: 12-15h;
ROA: p.o (2-3x0.25-0.5mg)
Nitrazepam
MOA: GABAA-R agonist;
IND: sleep disorders, insomnia;
SEs: sedation, amnesia, dependance, tolerance, sleeping patterns are not physiological;
Extra: short acting, hepatic metabolism;
ROA: p.o
Midazolam
MOA: GABAA-R agonist;
IND: anesthesia (i.v.), preoperative sedation;
SEs: sedation, amnesia, dependance, tolerance, sleeping patterns are not physiological;
Extra: fast onset, short active metabolite, ultra-short-acting, hepatic metabolism;
DOA: 1.5-2h;
ROA: p.o, i.v, i.n, i.m, s.c
Flumazenil
MOA: GABAA-R antagonist (at BDZ binding site);
Extra: rapid onset, short duration, also effective for terminating activity of zolpidem and zalplon;
IND: reverses effect of BDZs in sedation/anesthesia + overdose of BDZs;
ROA: i.v