Term
|
Definition
| anxiolytic- reduces aniety nad has calming effect |
|
|
Term
|
Definition
| sleep promoting drugs. Same cns effects promoting sedation, promote hypnosis, but to agreater degree. |
|
|
Term
|
Definition
|
|
Term
| benzodiazipines prototypic drug |
|
Definition
|
|
Term
|
Definition
high LIPHOPHILLICITY, rapid absorp in blood, easy penetaration into CNS. Also as a consequence easily cross placenta . Breast milk too!
clorazepate- only prodrugconverted to active form .
ACT FAST AND LAST LONG |
|
|
Term
|
Definition
entirly liver. CYP enzymes- particularly CYP3a4.
phase I metabolites arestill biologically active.
excretd entirely throug hthe kidney= phase II reaction is glucorindation to create hydrophillic molecules. |
|
|
Term
|
Definition
| useful for acute anxiety attacks, rather than long term, due to cumulative effects iwth multiple doses. can be useds for many types of anxiety |
|
|
Term
|
Definition
| mainly via kideny, but reducedk idney fucntion has no effect on reduced clearance |
|
|
Term
| other factors affecting benzo disposition |
|
Definition
| disease drug induced changesi n hepatic function, . Age- clearnece reduced as get older. Long Term Exposure will NOT induce or inhibit liver enzymes |
|
|
Term
|
Definition
| bind to GABAa receptors, activating the channel. BZ binding site occurs at a single spot- between alpha and gamma subunits (different from site from GABA). They are gabaergic drugs- increase FREQUENCY that GABA gated channel opening. |
|
|
Term
| benzos organlevel effects |
|
Definition
Sedation- acommopanies by depressant effects on psychoomotor and cognitive impairment.
Can cause disinhibitory effect- loss of self control.
Anterograde amnesia on DOA of drug.
Hypnosis can be promoted.
Stage III anesthesia at high doses.
4. some bzs hav anticonvsulant effe cts without significant cns depression
5. benzos- muscle relaxation- at higher than anxiolytic doses, depress skeletal enuromuscular jucntion.
6.respiratory and cardio derpession- in OD, takes alot. however watch for patietns who already have cardiopulm diseases |
|
|
Term
|
Definition
| rapid onset of action, realitvely high tehrapuetic index, avaialabilty of flumenil as antagonist. low risk of interactions. minimal effects on cardio and atuonmic functions |
|
|
Term
|
Definition
DEPENDANCE, depression of CNS functions (highly additive with other drugs, including alcohol).
Amensiac effects. |
|
|
Term
| benzos dosing considerations |
|
Definition
| use for SHORT TERM, in elderly , use half the dosage. Avoid combos. |
|
|
Term
|
Definition
| sedative/amensiac for surgical procedures. manage withdrawal from ehtanol. central muscle relaxants, derpession of delirium tremens |
|
|
Term
|
Definition
drowsiness , imapired judgement , diminished motor skills. Anterograde amnesia- , can look like ethanol intox
tolerance, psychological and physiolgoical depepndance can occur iwth long term use. Withdrawal symptoms can occur. Always make sure to taper dose. |
|
|
Term
|
Definition
| sedative=hypnotics most frequently used for itnentional ODs. BZs aresafer due to flat response curve. Respiratory depression, aspiration of contents, and choking. Cardio depression. |
|
|
Term
|
Definition
| ensure patent aireway, plasma volume, renal out put and cardiac function. |
|
|
Term
|
Definition
binds to GAba receptor- competitive inhibitor. Immediate reversal of BZ and new sleeping agents effects, dissapears quickly too. Repeated adminsitaritonmay be reuqierd due ot short half life.
Adverse efefcts: withddrawal symptoms from Bz dependance. |
|
|
Term
| benzos adverse effects urnelated to cns actions |
|
Definition
| some skin rashes, Teratogenic! |
|
|
Term
| buspirone MOA and effects |
|
Definition
purely anxiolytic, not hynptoic purposes. May be able to block withdrawal symptosm of benzos. Used for GAD and chronic anxiety, but not effective in treating panic disorders (takes too logn to work)- NOt useful for acute.
targets Ht1a receptors, and D2 receptors. as a partial agonist. |
|
|
Term
| buspirone adverse effects |
|
Definition
| NO tolerance develops, NO rebound anxiety or withdrawals. Less psychomotor imparients than BZ. However takes at least a week for anxiolytic effects to become established. |
|
|
Term
|
Definition
| raipdly absorbed, extensive first pass but with active metabolites. Super short halflife (2-4 Hours). emtabolized by cyp3a4. |
|
|
Term
| buspirone drug itneractio |
|
Definition
| MAOi- may elevate blodo rpessure. However anticholinergics ,alcohol etc. al lthe other stuffy ou cant take iwth benzos yo ucan take with this. |
|
|
Term
|
Definition
| are used for symptomatic side effectw of anxiety. - good for short term one shot deal. |
|
|
