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Benzo Anxiety , panic attacks, sedative hypnotic, agoraphobia |
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Benzo Anxiety, sedative hynotic |
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Benzo Anxiety, panic attack, preanesthetic medication, skeletal muscle relaxant, status epilepticus, w/drawl from alcohol, sedatives and hympnotics **very long acting drug MOA for muscle relaxant: decrease the potentiation of the GABA-A in the SC on 1st order neurons. DECRASES THE RELEASE OF THE EXCITATORY NTs. |
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Definition
Anxiety, panic attack, preanesthetic medication, skeletal muscle relaxant, status epilepticus, w/drawl from alcohol, sedatives and hympnotics, tremor |
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Definition
Preanesthetic medication ***very short half life |
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Definition
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Definition
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benzodiazepine characteristics |
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Definition
attach between the a and g subunit |
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Definition
increase in lipid = faster onset of action = shorter duration |
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Definition
Ligand gated ion channel acted on by benzos, barbs, alcohol and general anesthetics |
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Definition
GPCR (dimer) acted on via baclofen |
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Pharmological effects of benzos |
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Definition
1. decrease anxiety 2. hypnosia (onset and duration of sleep) 3. anticonvulsant 4. muscle relaxant 5. anterograde amnesia 6. interferes with learning and memory 7. additive or more effect with other CNS depressants |
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Benzo effect on respiration |
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Definition
1. none at normal doses 2. may suppress resp in pts with sleep apnea or chronic LD 3. may need resp assistance if combined with other CNS downers |
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Benzo effects on CV system |
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Definition
1. minor unless big ass OD 2. At preanesthetic concs--decr bp, incr HR 3. norm doses may cause CV depr in hypovolemics, CHF or general CV impairment. |
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Definition
Oral: best absorb. at high pH of SI Parental: irregular abs with IM; diazepam IV =pain + thrombophlebitis |
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Definition
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Long acting active metabolites (P1 and p2) |
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Definition
Clorazepate, Diazepam, Flurazepam t1/2= 24-100hrs (metabs often have half hours longer than parent) |
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Short Acting Active metabolites (P1 and 2) |
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Definition
Alprazolam, Midazolam, Triazolam t1/2=3 -18 hours a-hydroxylation and conjugation |
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Short Acting Active Metabolites (p2) |
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Definition
CONJUGATION ONLY Lorazepam, Temazepam |
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Random facts about old people |
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Definition
Elimination prolonged in old people because of the increased fat to TBW, e.g. volume of distribution increases |
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Inhibition of BEnzo metabolism by: |
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Definition
1. cimetidine 2. Whore pills 3. Isoniazid 4. Grapefruit Juice |
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Side Effects, toxicities and other reasons I hope I don't become a head case and need to take benzos (common) |
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Definition
Drowsiness (no tractor driving), sedation, impaired motor coord, wkns, dizzy, confusion, memory loss. ****tolerance to these develops ***SEs are an extension of desired actions |
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Definition
hallucinations paradoxical rage--excitement, stimulation and hyperactivity |
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Drowsiness, ataxia **additive with other downers |
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COUNTERINDICATED Not during pregnancy, delievery or breast feeding. Concentration in fetus ends up being higher than in mom. |
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Definition
bind benzo site on GABA but w/o Cl- channel opening. Also hinders inverse agonists |
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Definition
An imidazobenzodiazepine Reverse the sedative effect of benzo after anesthesia or in ODs. *Precipitates w/drawl T1/2= uno hour **cleared by liver, metabolized and excreted in the urine |
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Term
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Definition
develops to the antiC and hypnotic effects w/ chronic usage little tolerance to anxiety cross tolerance with other downers |
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Definition
little if any SCHEDULE IV DRUG DC'ing after LT use will result in sympton recurrence, rebound or w/drawl rxns |
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Definition
loss of effectiveness of the drug (more drug is needed to give same effect) |
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Definition
altered physio state that requires continuous drug admin to prevent the appearance of w/drawl sx. |
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Definition
increased CNS stimulation--convulsions **lesser degree with longer acting meds |
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sx are similar to those the pt experience prior to thx |
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sx are similar to what was experience b/f but with greater in tents city. **longer t1/2= longer till onset of sx. longer use = faster onset of sx. |
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sx. similar to rebound Sx. include: general anxiety, ANS signs--tachy, GI distress, mild HTN, sweating; Flu-like sx--m. ache, malaise; Sensory disturbances--photophobia, sound paresthesia, metallic taste; seizures and delirium |
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Definition
taper doeses by 25% a week |
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Definition
ability of one drug to suppress abstinence sx from a discontinuance of another drug. **use a longer acting drug to pv sx of withdrawl from a short acting one |
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Psychological vs. physiological dependence |
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Definition
Psych. more common, can occur at any dose |
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Definition
Generalized Anxiety--not other types partial agonist at 5-HT1A. Advantages over benzos: little sedative/euphoric effect, no rebound on abrupt stop, no potentiation of other downers. Disadvantage: a week for thx effect SE: tachy, palpitations, nervousness, GI distress, paresthesias (all more common than with benzos. |
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Definition
Sedative and Hypnotic Toxic/Anesthetic Doses 1. ↓ vasomotor center 2. ↓respirations (primary cause of death) 3. ↓ thermo center **Additive with other downers |
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Definition
absorbed readily via any route |
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Related to lipid solubility |
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