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Benzos
2nd test of 2009 M2
43
Women's & Gender Studies
Kindergarten
01/26/2009

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Cards

Term
Alprazolam
Definition

Benzo

Anxiety , panic attacks, sedative hypnotic, agoraphobia

Term
Clorazepate
Definition

Benzo

Anxiety, sedative hynotic

Term
Diazepam
Definition

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.

Term
Flurazepam
Definition
Benzo Insomnia
Term
Lorazepam
Definition
Anxiety, panic attack, preanesthetic medication, skeletal muscle relaxant, status epilepticus, w/drawl from alcohol, sedatives and hympnotics, tremor
Term
Midazolam
Definition
Preanesthetic medication ***very short half life
Term
Temazepam
Definition
Insomnia
Term
Triazolam
Definition
Insomnia
Term
benzodiazepine characteristics
Definition
attach between the a and g subunit
Term
CNS drug properties
Definition
increase in lipid = faster onset of action = shorter duration
Term
GABA-A
Definition
Ligand gated ion channel acted on by benzos, barbs, alcohol and general anesthetics
Term
GABA-B
Definition
GPCR (dimer) acted on via baclofen
Term
Pharmological effects of benzos
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

Term
Benzo effect on respiration
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

Term
Benzo effects on CV system
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.

Term
benzo abs
Definition

Oral: best absorb. at high pH of SI

Parental: irregular abs with IM; diazepam IV =pain + thrombophlebitis

Term
Benzo metabolism
Definition
NEEDED FOR ELIMINATION
Term
Long acting active metabolites (P1 and p2)
Definition

Clorazepate, Diazepam, Flurazepam

t1/2= 24-100hrs (metabs often have half hours longer than parent)

Term
Short Acting Active metabolites (P1 and 2)
Definition

Alprazolam, Midazolam, Triazolam

t1/2=3 -18 hours

a-hydroxylation and conjugation

Term
Short Acting Active Metabolites (p2)
Definition

CONJUGATION ONLY

Lorazepam, Temazepam

Term
Random facts about old people
Definition
Elimination prolonged in old people because of the increased fat to TBW, e.g. volume of distribution increases
Term
Inhibition of BEnzo metabolism by:
Definition

1. cimetidine

2. Whore pills

3. Isoniazid

4. Grapefruit Juice

Term
Side Effects, toxicities and other reasons I hope I don't become a head case and need to take benzos (common)
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

Term
SE of Benzos (uncommon)
Definition
hallucinations paradoxical rage--excitement, stimulation and hyperactivity
Term
Benzo toxicity signs
Definition

Drowsiness, ataxia

**additive with other downers

Term
Benzo's and pregnancy
Definition

COUNTERINDICATED

Not during pregnancy, delievery or breast feeding. Concentration in fetus ends up being higher than in mom.

Term
Benzo antagonists
Definition
bind benzo site on GABA but w/o Cl- channel opening. Also hinders inverse agonists
Term
Flumazenil
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

Term
Benzo Tolerance
Definition
develops to the antiC and hypnotic effects w/ chronic usage little tolerance to anxiety cross tolerance with other downers
Term
Benzo Dependence
Definition

little if any

SCHEDULE IV DRUG

DC'ing after LT use will result in sympton recurrence, rebound or w/drawl rxns

Term
Definition of tolerance
Definition
loss of effectiveness of the drug (more drug is needed to give same effect)
Term
Definition of dependence
Definition
altered physio state that requires continuous drug admin to prevent the appearance of w/drawl sx.
Term
Withdrawl Sx from Benzos
Definition

increased CNS stimulation--convulsions

**lesser degree with longer acting meds

Term
Def of Sx recurrence
Definition
sx are similar to those the pt experience prior to thx
Term
Def of Rebound
Definition

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.

Term
Def of W/Drawl
Definition

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

Term
Tx of withdrawl
Definition
taper doeses by 25% a week
Term
Cross dependence
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

Term
Psychological vs. physiological dependence
Definition
Psych. more common, can occur at any dose
Term
Buspirone
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.

Term
CNS Effects of Barbs
Definition

Sedative and Hypnotic

 

Toxic/Anesthetic Doses

1. ↓ vasomotor center

2. ↓respirations (primary cause of death)

3.  ↓ thermo center

 

**Additive with other downers

Term
Barb absorption MOA
Definition
absorbed readily via any route
Term
Barb onset of action
Definition

Related to lipid solubility

 

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