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40 Cards in this Set
- Front
- Back
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BENZODIAZEPINES
MAO |
-enhances action of GABA (inhibitory)
-causes ↑ chloride influx into neurons -cannot mimic GABA |
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BENZODIAZEPINES
PHARMACOKINETICS |
-lipid soluble
-extensive hepatic metabolization -creates metabolites that persist & continue to exert effects |
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BENZODIAZEPINES
CNS EFFECTS |
-CNS depression
- anti anxiety: limbic system -sleep: cerebrum -muscle relaxation- cerebellum & motor cortex |
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BENZODIAZEPINES
CARDIOVASCULAR EFFECTS |
-hypotension when given parenterally
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BENZODIAZEPINES
REPIRATORY EFFECTS |
-minimal depression compared to barbiturates
-be problem in pt with respiratory disorders |
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BENZODIAZEPINES
uses |
-anxiety: anxiolytic
-insomnia: hypnotic -seizure disorders -induction -conscious sedation -muscle spasm: Valium -panic disorder -alcohol withdrawal |
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BENZODIAZEPINES
ADVERSE EFFECTS |
-CNS depression
-anterograde amnesia -“sleep walking” -paradoxical effects: anxiety -respiratory depression -abuse: low -teratogenic |
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BENZODIAZEPINES
DRUG INTERACTIONS TOLERANCE |
-CNS depressants
-seizure disorders |
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BENZODIAZEPINES
PHYSICAL DEPENDENCE |
-withdrawal uncommon, but include anxiety & insomnia
-severe cases: seizures possible |
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BENZODIAZEPINES
TOXICITY |
-intravenous toxicity can lead to hypotension & respiratory depression
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Midazolam
trade type |
Versed©
Benzodiazephines |
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Midazolam
INDICATIONS |
-induction
-seizure -conscious sedation -sympathomimetic overdose |
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Midazolam
CONTRA |
-hypersensitivity
-myasthenia gravis (diagram in notes) -hypotension |
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Midazolam
Dose |
Induction: 0.1mg/kg IVP (max single 5mg)
Maint: 2.5mg IVP q 10 min PRN Seizure: 10mg IM (max total 10 mg) or 5mg IV (max total 20mg) Conscious Sedation 0.05mg/kg IVP (max single 2.5mg) Combative Behavior 5-10mg IM (max total 10mg) or 2.5-5mg IV (max total 10mg) Sympathomimetic Overdose 10mg IM (max total 20mg) or 5mg IV (max total 20mg) |
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Lorazepam
trade type |
Ativan©
Benzodiazepines |
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Lorazepam
INDICATIONS |
-acute anxiety
-alcohol withdrawal -seizure |
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Lorazepam
CONTRA |
-hypersensitivity
-acute narrow-angle glaucoma |
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Lorazepam
Dose |
Alcohol withdrawal 1mg SL (max total 2mg)
Acute Anxiety 1mg SL (max total 2mg) Seizure 2-4mg IV or IM |
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Diazepam
trade type |
Valium©
Benzodiazepines |
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Diazepam
Indications |
-muscle spasm
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Diazepam
CONTRA |
-hypersensitivity
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Diazepam
Dose |
2.5-5mg IVP (max total 20mg)
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Flumazenil
Trade type |
Anexate©
Benzodiazepine Antagonists |
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Flumazenil
used |
-given to reverse Benzodiazepine OD
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Flumazenil
MAO |
-competitive Benzodiazepine Antagonist
-greater effects on CNS depression, less on respiratory depression |
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Flumazenil
CONTRA |
-mixed OD
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Flumazenil
PRECAUTIONS |
-seizure disorders
-benzodiazepine dependence |
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Flumazenil
dose |
1ST: 0.2mg over 30 sec, wait 1 min
2nd: 0.3mg over 30 sec, wait 1 min 3rd: 0.5mg over 30 sec, wait 1 min Subsequent doses: 0.5mg (max total 3mg) |
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Barbiturates
Classification |
Ultra Short Acting - Thiopental - Induction
Short-Intermediate Acting - Secobarbital - Sedative/Hypnotic Long Acting - Phenobarbital - Seizure |
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Barbiturates
Mechanism of Action |
Enhance GABA
Mimic GABA |
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Barbiturates
CNS Effects |
Non-specific depression
Phenobarbital is the exception |
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Barbiturates
Cardiovascular Effects |
Hypotension
Bradycardia |
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Barbiturates
Hepatic Effects |
Stimulate the synthesis of drug metabolizing enzymes
Causes an increase in metabolism of itself and other drugs |
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Barbiturates
Tolerance |
Tolerance develops to therapeutic effects such as sedation and hypnosis.
However tolerance to toxic effects such as respiratory depression remain the same. As dosing is increased to reach therapeutic effects, it becomes closer and closer to toxic effects. |
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Barbiturates
Physical Dependence |
General CNS depressants carry one of the greatest risks for serious withdrawal manifestations.
Cross dependence and longer acting barbiturates allow for possible withdrawal relief. |
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Barbiturates
Pharmacokinetics |
Dependant upon degree of lipid solubility
All barbiturates other then the highly lipid soluble have very long half lives. This causes accumulation, tolerance, and residual effects |
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Barbiturates
Uses |
Seizure Disorders - Phenobarbital
Induction - Thiopental Insomnia |
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Barbiturates
Adverse Effects |
Respiratory Depression - Brainstem/Chemoreceptors
Suicide Abuse Teratogenic Paradoxical Excitement Hyperalgesia |
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Barbiturates
Drug Interactions |
CNS Depressants
Hepatic Metabolization - Warfarin, Oral Contraceptives, Phenytoin |
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Barbiturates
Toxicity |
The Clinical Triad…
CNS Depression Respiratory Depression Pinpoint Pupils Narcan does NOT reverse this type of OD The drug must be removed through gastric lavage or hemodialysis Respiration must be supported |
