| Question |
Answer |
| Benzodiazepines are most commonly used ____________ medication |
anti-anxiety |
| They are also grouped in ____________ medication |
sedative-hypnotic |
| They are also classified as centrally mediated ____________ ____________ |
muscle relaxants |
| Mechanism of action: CNS depression specific to the areas in ____________, _________ and ______ system of the brain |
hypothalamic, thalamic, limbic |
| Indications |
anxiety relief, sedation, anticonvulsant, muscle relaxants, appetite stimulant, retrograde amnesia |
| Sedative effects through depression of |
limbic system |
| Muscle relaxing effect via inhibiting of the ______ at the spinal level |
internunical neurons |
| There are two major inhibitory amino acid neuro transmitters in the CNS= |
glycine and gamma-amino-butyric acid (GABA) |
| _______ performs inhibitory function in the spinal cord, brain stem and retina. |
glycine. |
| GABA is found in the __________ and _________ |
cerebrum and cerebellum |
| Benzodiazepines action is through _________ of specific (BZ) receptors |
stimulation |
| There are as many as __________ variations of BZ receptors |
6 |
| How many categories of action can be identified |
3 |
| Agents which _________ _________ bindings and - induced ___________ current are known agonist. |
increases GABA, chloride |
| Drugs that reduce ______ ______ binding and induce _______ _______ are known as inverse agonists. |
both GABA, chloride influx |
| Drugs that reduce both GABA and induce Chloride influx are known as |
inverse agonists |
| inverse agonists are responsible for |
anxiety, convulsion and analeptic properties |
| The third group the genuine antagonist of both agonist and inverse agonist are drugs that bind but have no efficacy at the site, _________ is a drug of this type |
flumazenil |
| How many types of GABA receptors are found at pre and post synaptic site |
2 |
| what are the GABA type of receptors found at pre and post synaptic site. |
A & B |
| Important to remember is that Benzodiazepines potentates the action of __________ and increases the frequency of _________ channel opening. |
GABA, Chloride (Cl) |
| Benzodiazepines derivatives are |
Diazepam, Midazolam, Chloradiazepoxide, Lorazepam, Alprazolam, Clonazepam, Zolazepam, Chlodiazepam. |
| Which Benzodiazepines are used in Veterinary Medicine |
Diazepam, Midazolam, Zolazepam, Chlodiazepam |
| What are the common names for BZ used in Veterinary Medicine |
Valium, Versed, Zolazepam, Chlodiazepam |
| How many BZs are we learning about |
8 |
| How many BZs are used in Veterinary Medicine |
4 |
| What is the acronym for the BZs use in Vet Med. |
DMZC |
| Name for Diazepam |
Valium |
| Name for Midazolam |
Versed |
| Name for Chloradiazepoxide |
Librium |
| Name for Lorazepam |
Ativan |
| Name for Alprazolam |
Xanax |
| Name for Clonazepam |
Klonopin |
| This drug is insoluble in water, solution contains solvent propylene glycol, ethanol and sodium benzoate in benzoic acid |
Diazepam |
| IV injection of __________ can cause thrombophlebitis. |
Diazepam |
| Can Diazepam be used orally? |
Yes |
| Which of these can Diazepam pass through? the blood-brain barrier or placental barrier |
Both |
| What percent of Diazepam is protein bound |
almost 90% |
| Diazepam's half life is |
6 to 21 hours |
| How is diazepam metabolized |
in the liver by demethylation and hydroxylation |
| In the liver diazepam is demthylated and hydroxylated to how many forms |
3 |
| what are the active forms of diazepam demethylated and hydroxylated by the liver |
N-demethyldiazepam, 3-hydroxydiazepam and oxazepam |
| Diazepam metabolites are conjugated to ________ by the liver. |
glucuronide |
| Glucuronide is excreted by |
Kidneys |
| Is the toxcity of Diazepam low or high |
low |
| How do you treat an overdose of Diazepam |
with flumazenil |
| Clinical Uses for Diazepam include |
convulsion control, used in dog, cat, horse to prevent post-op convulsion caused by use of contrast media into spinal cord for radiography, premedication for sedation, etc |
| Diazepam has been used as muscle relaxation with what other drugs to perform minor surgical procedures |
ketamin, xylazine, opiods, etc |
| This drug is water soluble and not painful given IV |
Midazolam |
| Midazolam is metabolized by |
the liver |
| what is the half life of Midazolam |
shorter than Diazepam |
| Midazolam effects on repiratory and cardivascular are |
minimal like others in the group |
| Midazolam are used widely with combinations of |
opioids |
| Does Midazolam readily cross the blood-brain barrier |
yes |
| which is more potent Midazolam or Diazepam |
Midazolam |
| Midazolam clinical uses include |
anticonvulsant, muscle relaxant, appetite stimulant |
| what is the acronym for Midazolam clinical uses |
the AMA |
| Midazolam is combined with |
ketamine and other anesthetics |
| Diazepam and Midazolam can cause what type of changes in dogs and cats |
behavior |
| Midazolam can cause these animals restless, to pace, vocalize, and difficult to approach |
cats |
| can midazolam cause an increase or decrease in food consumption |
increase |
| what drug antagonizes the effects of all benzodiazepines |
flumazenil |
| what is another name for flumazenil |
romazicon |
| what action speed of flumazenil |
rapid 2 to 4 minutes |
| Reversal by flumazenil is or is not accompanied by anxiety and cardiovascular effects |
is not |
| how long does the antagonistic effects of flumazenil effects last |
about 60 minutes |
| should you ever redose flumazenil |
yes it may be required |
| Zolazepam is sold in combination with |
tiletamine |
| in what ration is zolazepam and tiletamine sold in |
1 : 1 |
| what is the combination of zolazepam and tiletamine called? |
telazol. |
| Telazole contains what |
250mg of zolazepam and 250mg of tiletamine |
| tiletamine is a dissociative agent similar to |
ketamine |
| Telazole is widely used in |
ruminants |