Term
|
Definition
Sedation: Decrease in activity, moderation of excitement
calming |
|
|
Term
|
Definition
Hypnosis: drowsiness, a state that facilitates the onset of
“natural” sleep. Not to be confused with the
induced state of passive suggestibility |
|
|
Term
|
Definition
| Anxiolysis: decrease in anxiety level |
|
|
Term
| When should go give sedatives/hypnotics? |
|
Definition
1. Anxiety disorders
2. Convulsive disorders
3. Insomnia
4. Sedation for medical procedures or
preoperative
5. Component of balanced anesthesia
6. Muscle relaxation |
|
|
Term
|
Definition
Dose dependent depression of the CNS except
Phenobarbital;
Poor anxiolytics - more pure sedative;
Good for induction of general anesthesia: thiopental |
|
|
Term
|
Definition
| potentiates inhibatory qualities of GABA A receptors (by enhancing binding of GABA to GABA A receptor) and inhibits excitatory AMPA receptors |
|
|
Term
| How do Bars enhance binding of GABA to GABA receptors? |
|
Definition
Increases chloride current with GABA activation;
Depresses voltage gated Calcium currents |
|
|
Term
|
Definition
Gamma-aminoburtyric acid;
Most common inhibitory amino neurotransmitter |
|
|
Term
|
Definition
| Found all over the CNS, spinal cord and PNS |
|
|
Term
| What is the GABA receptor? |
|
Definition
Four transmembrane protein moieties repeated in five groups
that surround a central chloride channel. |
|
|
Term
| What does the GABA receptor do? |
|
Definition
Activation hyperpolarizes membranes which inhibits
the neuron from producing an action potential. |
|
|
Term
| How can it be disinhibited? |
|
Definition
| Disinhibition can come from inhibiting the inhibitory pathways |
|
|
Term
|
Definition
Decreases blood pressure by decreasing preload
(inhibits homeostatic reflexes) and by decreasing
the force of contraction (inotropy).;
Suppression of CO2 response curve and hypoxic
ventilatory drive. |
|
|
Term
| How are barbiturates metabolized? |
|
Definition
Hepatic metabolism by cytochrome p450. Can induce increased
production of p450 enzymes |
|
|
Term
|
Definition
| phenobarbital, thiopental, methohexital |
|
|
Term
| What are the major effects of Benzos? |
|
Definition
Sedation;
Hypnosis;
Anxiolysis;
Anticonvulsant;
Muscle relaxation;
Amnesia |
|
|
Term
| Are they safe when used as a single agent? |
|
Definition
| Very safe drugs when used as a single agent. |
|
|
Term
| What happens when the dose of benzos increases? |
|
Definition
As the dose of benzodiazepine is increased disinhibition
progresses to sedation then to to hypnosis and then to stupor.
Death from a pure benzodiazepine overdose is rare. |
|
|
Term
| What are the cardiovascular/resp effects? |
|
Definition
Mild decreases in blood pressure which causes a
barroreceptor mediated increase in heart rate.
Possible mild negative inotropes.
Mild dose dependent effects on central initiation
of respiration. May be significant in patients
with severe lung disease. |
|
|
Term
| What are the mech of action of Benzos? |
|
Definition
Directly bind to GABA receptor/chloride channel complex
and increases chloride current when the receptor is
activated by GABA.
Chloride current hyperpolarizes membranes and inhibits the
neuron from producing an action potential.
Differential binding to GABA subtypes/populations causes
differences in clinical effect. |
|
|
Term
|
Definition
| Diazepam (valium), midazolam, flumazenil, zolpidem (ambien) |
|
|
Term
| What are anticholinergics? |
|
Definition
| OTC sleep aids, antidperessants/ |
|
|
Term
| What are side effects of Anti-Chol |
|
Definition
Significant potential problems:
Elderly: confusion and inability to urinate
Dry mouth, tachycardia, constipation |
|
|
Term
|
Definition
Overdose:
“dry as a bone, red as a beet, mad as a hatter”
Rx: physostigmine: allows acetylcholine to build up |
|
|
Term
| What type of side effects can benzos produces when used as sleep aids? |
|
Definition
Long-term hypnotics lead to decreased effectiveness.
Rebound insomnia may occur with withdrawal.
Benzodiazepines produce cognitive changes, alter sleep architecture, cause morning drowsiness and motor impairment. |
|
|
Term
| When should you use a benzo to sleeep? |
|
Definition
| Benzodiazepines may be best choice for patients with insomnia and anxiety disorder |
|
|
Term
| What is chronic injection of ETOH a marker for? |
|
Definition
| psychological disturbance |
|
|
Term
| What does chronic EtOH ingestion do? |
|
Definition
Serious neurologic and psychiatric disorders;
Toxicity to heart muscle causes heart failure;
Liver damage causes cirrhosis;
Bone marrow damage causes anemia;
GI damage causes ulcers;
Fetal alcohol syndrome |
|
|
Term
| When do you use EtOH theraputicall? |
|
Definition
Alcohol is in many OTC medications
Neurolytic procedures for treatment of cancer pain |
|
|
Term
| How does EtOH effect sedative/hypnotics? |
|
Definition
Acute ethanol intoxication increases the effect of sedatives
and hypnotics. It is often a deadly combination. |
|
|
Term
| How does EtOH alter clearance? |
|
Definition
Alters clearance of many drugs including phenytoin and
oral hypoglycemics. |
|
|
Term
| How does EtOH shorten drug effectiveness? |
|
Definition
Chronic ethanol ingestion increases liver oxidative function
(assuming no cirrhosis) and can shorten drug effectiveness. |
|
|
Term
| How do you treat EtOH OD? |
|
Definition
Insure safety of patient: ABC’s, warmth, aspiration prophylaxis
IV fluids with thiamin and multivitamins prior to any glucose
containing fluids. Prevents Wernicke’s encephalopathy.
Benzodiazepines reduce risk of alcohol withdrawal seizures |
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