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Benzodiazepine

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Andrea gorin

on 22 August 2013

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Transcript of Benzodiazepine

Benzodiazepine
By: Andrea Gorin, Cody Hart, & Katie Nolin
Discontinuation
All benzodiazepines precipitate withdrawal symptoms during discontinuation. These may range from mild to severe, depending on the method of weaning/discontinuation used.

Discontinuation should be done slowly over a period of weeks/months. Withdrawal Symptoms may range from:
(1) Epileptic seizures
(2) Myoclonic jerks
(3) Paranoid psychotic symptoms
(4) Delirium
(5) Visual/Auditory hallucinations
(6) Depersonalization
(7) Nausea
(8) Anorexia
(9) Persistent headaches
(10) Tremors
(11) Palpitations
(12) Sweating
(13) Influenza-like symptoms.


Benzodiazepines are generally rapidly and fully absorbed after oral ingestion with peak plasma concentrations occurring from 0.5 to 2 hours after administration. There are some differences in
absorption rate between the various drugs. They are metabolized both by oxidation which may produce active compounds, and by glucuronidation which inactivates them. They differ widely in their rate of removal from the body.
Therapeutic Monitoring & Interaction with other drugs
Use of benzodiazepines reduces the need for the natural brain production of GABA. As production of GABA is reduced, the need for artificial supplementation increases (benzos). All benzodiazepine use can develop into a tolerance after several days and all use carries a significant risk of dependence after several weeks.
Typical Doses
Benzodiazepines (BDZs) A group of
structurally related compounds that
have sedative properties. Because of
their greater safety margin, BDZs
have, for the most part, replaced the
barbiturates, a more dangerous class
of sedatives
GABA Video
Toxicity & Side Effects
Indications for Use
outbursts of anger
depression
hallucinations
low blood pressure
skin rash/itching
fever & chills
sores in the throat/mouth
unusual bruising/bleeding
extreme fatigue
Avoid driving, pregnancy & alcohol
low risk when used solely
CNS Depression
lethargy
slurred speech
ataxia
coma
respiratory
Should not be combined w/ drugs that inhibut the CNS

Theoretical Rationale
Benzodiazepines act by potentiating the action of gamma-aminobutyric acid (GABA) at the GABA receptor.
Interaction with the benzodiazepine receptor results in neuronal inhibition and inhibitory effects on the centralnervous system (CNS). Most differences between benzodiazepines are explicable in terms of different pharmacokinetic properties
Advantages of use
high efficacy
rapid onset of action
low toxicity
Relief of anxiety symptoms
Induce sleep
antiepileptic actions
reduction of myoclonus
skeletel muscle relaxant
amnesic effects
The various benzodiazepines and their respective trade-names, half-lives, primary uses and benzodiazepine equivalent doses are listed in the following table.
Drug Name Common Brand Names Time to Peak (Onset of action in hours) Elimination Half-Life (h) [active metabolite] Primary Effects Approximate Equivalent Dose
Alprazolam Xanax, Xanor, Tafil, Alprox, Frontal (Brazil) 1-2 6-12 hours anxiolytic 0.5 mg
Bromazepam Lexotanil, Lexotan, Lexomil, Somalium, Bromam 1-3 10-20 hours anxiolytic 5-6 mg
Chlordiazepoxide Librium, Tropium, Risolid, Klopoxid 1.5-4 5-30 hours [36-200 hours] anxiolytic 25 mg
Cinolazepam Gerodorm .5-2 9 h hypnotic 40 mg
Clonazepam Klonopin, Klonapin, Rivotril, Iktorivil 1-4 18-50 hours anxiolytic, anticonvulsant 0.5 mg
Cloxazolam Olcadil (Brazil) 2-5 (?) 18-50 hours anxiolytic, anticonvulsant 1 mg
Clorazepate Tranxene Variable [36-100 hours] anxiolytic, anticonvulsant 15 mg
Diazepam Valium, Apzepam, Stesolid, Vival, Apozepam, Hexalid, Valaxona 1-2 20-100 hours [36-200] anxiolytic, anticonvulsant, muscle relaxant 10 mg
Estazolam ProSom 0.5-5 10-24 h hypnotic 1-2 mg
Flunitrazepam Rohypnol, Fluscand, Flunipam, Ronal, Rohydorm (Brazil) 0.5-3 18-26 hours [36-200 hours] hypnotic 1 mg
Flurazepam Dalmadorm, Dalmane 1-1.5 [40-250 hours] hypnotic 20-25 mg
Flutoprazepam Restas 0.5-9 60-90 hours hypnotic 2-3 mg
Halazepam Paxipam 1-3 [30-100 hours] anxiolytic 20-40 mg
Ketazolam Anxon 2.5-3 30-100 hours [36-200] anxiolytic 15-30 mg
Loprazolam Dormonoct 0.5-4 6-12 hours hypnotic 1-2 mg
Lorazepam Ativan, Temesta, Lorabenz 2-4 10-20 hours anxiolytic,anticonvulsant 1 mg
Lormetazepam Loramet, Noctamid, Pronoctan 0.5-2 10-12 hours hypnotic 1-2 mg
Medazepam Nobrium ? 36-200 hours anxiolytic 10 mg
Midazolam Dormicum, Versed, Hypnovel, Dormonid (Brazil) 0.5-1 3 hours (1.8-6 hours) hypnotic 5 mg
Nimetazepam Erimin 0.5-3 14-30 hours hypnotic 5 mg
Nitrazepam Mogadon, Alodorm, Pacisyn, Dumolid 0.5-7 15-38 hours hypnotic 10 mg
Nordazepam Madar, Stilny ? 50-120 hours anxiolytic 10 mg
Oxazepam Seresta, Serax, Serenid, Serepax, Sobril, Oxascand, Alopam, Oxabenz, Oxapax 3-4 4-15 hours anxiolytic 30 mg
Phenazepam ? 1.5-4 60 hours anxiolytic, anticonvulsant 1 mg
Pinazepam Domar ? 40-100 hours anxiolytic 20 mg
Prazepam Lysanxia, Centrax 2-6 36-200 hours anxiolytic 10-20 mg
Premazepam 1 2-6 10-13 hours anxiolytic 3.75 mg
Quazepam Doral 1-5 39-120 hours hypnotic 20 mg
Temazepam Restoril, Normison, Euhypnos 0.5-3 8-22 hours,/p> hypnotic 20 mg
Tetrazepam Mylostan 1-3 3-26 hours Skeletal muscle relaxant 50mg
Triazolam Halcion, Rilamir 0.5-2 2 hours hypnotic 0.25 mg

Enumeration of Drugs
Should not be used with
Other drugs that inhibit the CNS (hypnotic agents, sedating antidepressants, neuroleptic agents, anticonvulsants, antihistamines)
Use with barbituates and other sedatives can increase sedation and depress breathing to dangerous levels.
Sleeping pills
References
Ashton, H. (1994). Guidelines for the rational use of Benzodiazepines: When and what to use. Drugs, 48(1), 25-40.
Michelle McGuire. (n.d.). Pharmacology of anxiety disorders [PowerPoint slides]. Retrieved from https://newclassroom3.phoenix.edu/Classroom/#/context/co/contextid/OSIRIS:39832882.
Mergel, M. (2011). Benzodiazepines. Retrieved from http://toxipedia.org/display/toxipedia/Benzodiazepines
Rankin, E. A. (2000). Quick Reference for Psychopharmacology. Albany, NY: Delmar Thomson Learning.
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