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71 Cards in this Set
- Front
- Back
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Benzodiazepine mechanism
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Bind GABA receptor alpha-subunit noncompetitively
Increase activity of GABA receptor activity when GABA is bound Bind receptor subtypes alpha 1, 2, 3, 5 |
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GABA receptor subtype alpha-2
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Binds anxiolytics
Predominant in limbic system, cortex and striatum |
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GABA receptor subtype alpha-1
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Binds sedatives
Most abundant subunit, widespread distribution |
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GABA receptor subtypes alpha-1,5
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Affects learning and memory
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Benzodiazepine structure
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- Benzene ring
- 7-membered diazepine ring - 5-aryl substituent ring |
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Benzodiazepine absorption and distribution
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Rapid and complete GI absorption
Lipophilic with rapid CNS effects Highly protein bound - widely distributed in body |
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Benzodiazepine metabolism and excretion
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Extensive hepatic metabolism, but minor effects on P450s
Half-lives (t1/2) can be divided into short-, intermediate- and long-acting Excreted in the urine as glucuronides |
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Alprazolam
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BZD
Xanax 9-20 hr t1/2 (intermediate) High potency |
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Clonazepam
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BDZ
Klonopin 19-60 t 1/2 (long) High potency |
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Lorazepam
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BDZ
Ativan 8-24 hr t1/2 (intermediate to long) |
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Triazolam
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BDZ
Halcion 1.5-5 hr t1/2 (Short) High potency |
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Benzoidazepine indications
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Anxiety, insomnia, convulsions/seizure, muscle strain, tonic-clonic seizure
Short acting: Insomnia Intermediate acting: Withdrawl seizures, grand mal seizures Long acting: chronic anxiety,sleep disorders |
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Benzodiazepine effects
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Sedation (tolerance develops)
Muscle weakness, weight gain, headache, blurred vision, joint pain Anterograde amnesia just after taking drug Supression of REM sleep, increases stage 2 sleep Effects enhanced with alcohol Cause birth defects |
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Benzodiazepine tolerance
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Pharmacodynamic - receptor-mediated tolerance
Decrease in receptor numbers |
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Benzodiazepine dependence
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More pronounced with short acting BDZs
Psychological and physical symptoms |
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Benzodiazepine toxicity
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Overdose leads to excessive sleep
Enhanced effects with alcohol may cause respiratory depression and death |
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Flunitrazepam
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BDZ
Date-rape drug Rohypnol Drowsiness, impaired motor skills and anterograde amnesia Schedule I compound |
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Gamma-hydroxybutyrate
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Date-rape drug
Loss of motor control, disinhibition, amnesia, intoxication, dizziness Used in Europe to treat narcolepsy Fatal if combined with alcohol |
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GABA alpha-3 subunit
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In Noradrenergic and serotonergic neurons of the brainstem reticular formation
Basal forebrain cholinergic neurons GABAergic neurons in the reticular nucleus of the thalamus |
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Zolpidem
Eszopiclone |
Non-BDZ sedative
Ambien/Lunesta Bind benzodiazepine site on GABA alpha-1 subunit t1/2 = 2-3 hours Metabolized in liver Cause sedation but no other defecits Minimal tolerance/dependence |
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Barbiturate indications
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Anesthesia
Insomnia Anti-convulsant Anxiety (Rarely used) |
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Barbiturate mechanism
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Bind barbiturate binding site on GABA-A
Increase activity of GABA receptor **At high doses may be GABA mimetic** |
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Phenobarbitol
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Barbiturate
80-120 hr t1/2 (long) Insomnia, preop, sedation, seizure |
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Barbiturate effects
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Sedation
Hypotension Respiratory suppression "Drug Hangover" Birth defects |
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Barbiturate dependence
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withdrawal from barbiturates may cause tremors, anxiety, weakness, restlessness, nausea and vomiting, seizures, delirium, and cardiac arrest.
**May be fatal** |
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Barbiturate tolerance
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Pharmacodynamic and pharmacokinetic tolerance develops with chronic use
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Barbiturate toxicity
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Low therapeutic index
Potentiated by alcohol and other sedative-hypnotics slow respiration, cyanosis, and greatly diminished Must maintain breathing and circulation |
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Buspirone
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"Buspar"
5-HT1A partial agonist Anxiolytic without hypnotic, anticonvulsant, and muscle relaxant properties No tolerance/dependence Allow 2 wks for onset t 1/2 = 2-3 hrs Paradoxical side effects (anxiety-like symptoms) Does not work for panic attacks |
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Other anxiolytics used
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SSRIs, TCAs, MAOIs
Propranolol, Clonidine |
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Vigabartin
(Sabril) |
Blocks breakdown of GABA by inhibiting GABA-T
(Increases GABA in brain) Used in conjunction w/ BZD |
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Tigabine
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Anticonvulsant
Inhbits GABA reuptake (Increases GABA in brain) Used in conjunction w/ BZD Causes nervousness/dizziness |
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Phentytoin
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Dilantin
Anticonvulsant Blocks Na channels just after they open to inhibit continued activity Side effects; gingivitis, acne, hirsutism |
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Carbamazepine
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Tegrol
Blocks Na channels just after they open to inhibit continued activity Side effects:hyponatremia, nutropenia |
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Ethosuxamide
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Zarontin
Anti-convulsant 1st med for absence seizures Blockade of T-type Ca channels used in thalamic reverberating activity Side effects: GI intolerance, hepatic toxicity |
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Valproate
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Depakote, Depakene
Anti-convulsant For all seizure types Mechanism: boosts GABA transmission and inhibits Na channels Side effects: hepatoxicity, weight gain, hair loss |
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Felbamate
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Felbatol
Anti-convulsant For ALL seizures |
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Gabapentin/Pregabalin
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Anti-convulsant
Neurontin/Lyrica For partial and secondarily generalized seizure May interact with voltage-gated Ca channels Indirect interaction with GABA receptors |
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Lamotrigine
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Lamictal
Anti-convulsant (NEW) For all seizures Inhibits Na and Ca channels Side effect: Steven-Johnson syndrome |
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Topiramate
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Topomax
Anti-convulsant (NEW) All seizure types |
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Levetiracetam
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Keppra
Anti-convulsant (NEW) For all seizure types |
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Oxycarbazine
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Trileptal
Anti-convulsant (NEW - derivative of carbamazepine) For partial seizures Inhibits Na channel activity |
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Zonisamide
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Zonegran
Anti-convulsant (NEW) All seizure types Inhibits Na and Ca channels Few side effects |
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L-DOPA
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Used to treat Parkinsons
Given with carbidopa |
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Carbidopa
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Given with L-DOPA to prevent AAAD from converting it to DA in the PNS
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Sinemet
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L-DOPA + carbidopa
For Parkinsons |
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L-DOPA side effects
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Nausea & vomiting
3. Cardiac stimulation 4. Loss of efficacy over time: neuronal degeneration 5. Psychosis |
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Other treatments to increase DA
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MAOIs
Dopamine receptor agonists: Bromocryptine Amantadine: increase DA release |
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Benztropine
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Decreases ACh to treat Parkinsons
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Phenothiazines
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Chlorpromazine (alliphatic)
Thioridazine (Piperidine) Trifluoperazine (Piperazine) |
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Chlorpromazine
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Weak antipsychotic
Phenothiazine Aliphatic side chain Not used at all - may be fatal |
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Thioridazine
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Moderate potency antipsychotic
Piperidine side chain Penothaizine Mellaril |
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Trifluoperazine
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High potency antipsychotic
Piperazine side chain Penothaizine |
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Haloperidol (Haldol®)
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Butyrophenone class
High potency typical antipsychotic |
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Atypical antipsychotics
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Clozapine
Olanzapine Risperidone |
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Clozapine
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Atypical antipsychotic
May cause fatal agranulomatous blood condition |
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Olanzapine
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Atypical antipsychotic
Highly potent antipsychotic Safer form of clozapine |
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Risperidone
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Atypical, potent antipsychotic
A D2 antagonist also potent at other receptors including 5-HT2, alpha-adrenergic and histamine H1 |
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Typical antipsychotic mechanism
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Bind D2 receptors antagonistically
Preferred drug screen was to induce vomiting, then block it with antipsychotics |
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Side effects of antipsychotics
(Non-DA dependent) (2) |
Drowsiness and orthostatic hypotension due to binding at alpha-1 receptors
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Side effects of antipsychotics
(DA dependent) (4) |
Parkinsonism
Tardive dyskinesia Anti-nausea Decreased seizure threshold |
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Drug choice consequences for psychosis
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Lower sedation = higher potency
Lower parkinsonism = weaker drug |
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Buproprion
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Wellbutrin
Antidepressant Nicotinic antagonist DA/NE reuptake inhibitor |
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Treatment for Panic Disorder/PTSD
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Benzodiazepines
SSRIs Beta blockers (treat symptoms) Cognitive behavior therapy Desensitization |
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Treatment for Generalized Anxiety Disorder
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TCAs
SSRIs Cymbalta Buspirone (few side effects) Beta blockers Antihistamines Benzodiazapines |
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Treatment for OCD
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Serotonin specific antidepressant (SSRI/clomipramine)
High doses of antidepressants |
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Dipyridamole
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Inhibits phosphodiesterase and adenosine reuptake
Combined with aspirin |
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Thienopyridine
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Antiplatelet agent
Reversibly inhibits ADP-induced exposure of fibrinogen binding site |
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Clopidrogrel
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Antiplatelet drug superior to aspirin in symptomatic patients
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Methylphenidate
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Drug class of Ritalin
For ADHD Block NE/DA reuptake (TCA) |
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Amphetamine
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Drug class for Adderall
For ADHD Increase NE/DA release and block reuptake |
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Lisdexamphetamine
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Prodrug of amphetamines for ADHD
Must be taken orally and go through portal system to be active Takes a while to become effective Combine with stimulant |
