Pharmacology
PHARMA BOARD
Anxiety
 Fear, apprehension and worry
 Accompanied by physical sensations such
as anxiety, nausea, chest pain and/or
sho...
Neurotransmitters
 Excitatory NTs
 Key words: sodium, calcium, depolarization
 Inhibitory NTs
 Key: chloride, GABA, hy...
Excitatory neurotransmitters
 opens Na or Ca channels/ influx
depolarization (more positive) nerve
impulse
 e.g. Norep...
Inhibitory neurotransmitters
 opens Cl channels hyperpolarization
(more negative)  no nerve impulse
 e.g. glycine, gam...
 1. Panic disorder- recurrent unexpected
panic attacks that can occur with
agoraphobia in which patients fear places
in w...
 3. Social phobia-intense fear of being
scrutinized in social or public situations
(e.g., giving a speech, speaking in cl...
 5. Post-traumatic stress disorder-
persistent reexperience of a trauma, efforts
to avoid recollecting the trauma, and
hy...
Sedatives-Hypnotics
 Benzodiazepines
 Increase the frequency of GABA-mediated
chloride ion channel opening
 Barbiturate...
Classes of Anxiolytic and Hypnotic
drug
Benzodiazepines
 5-HT1A-receptor agonists
 β-adrenoceptor antagonists
Benzodiazepines
 Act by binding to a specific regulatory site
on the GABA A-receptor
 enhances the inhibitory effect of ...
Receptor Empty
Intra cellular
GABA
GABA
Receptor
-
CL
+++++++
- - - - -
NaChannel
NaChannel
Intra cellular
GABA
GABA
Receptor
-
CL
+ + + +
- - - -
NaChannel
NaChannel
- - - -
Use of The Drugs
Clinical indications for the use of the
anxiolytics, sedatives and hypnotics
 1. Prevention of anxiety
...
ACTIONS
 Reduction of anxiety
 Sedative – hypnotics
 Anticonvulsant
 Muscle relaxant
The BENZODIAZEPINES
The benzodiazepines are the most frequently used
anxiolytic drugs.
These agents prevent anxiety states...
The BENZODIAZEPINES
 Long Acting
 Intermediate Acting
 Short Acting
Long Acting (1-3 days)
 Charlie Chaplein Died From Q-fever
Long Acting (1-3 days)
 Charlie - Chlorazepate
 Chaplein - Chlordiazepoxide
 Died - Diazepam
 From - Flurazepam
 Q-fe...
Intermediate
 L A T E
Intermediate
 L - Lorazepam
 A - Alprazolam
 T - Temazepam
 E - Estazolam
Short Acting
 O- Oxazepam
 T- Triamzolam
 Uses:
 Anxiety- alprazolam, diazepam
 Seizures- diazepam, clonazepam,
lorazepam
 Insomnia- flurazepam, midazolam
 Pr...
The BENZODIAZEPINES
Special uses
Diazepam
(Valium)
Status epilepticus
Chlordiazepoxide
(Librium)
Alcohol
withdrawal
Alpraz...
The BENZODIAZEPINES
These agents are indicated for the treatment of
1. anxiety disorders
2. alcohol withdrawal
3. hyperexc...
The BENZODIAZEPINES
Pharmacodynamics: The adverse effects
 CNS effects= drowsiness,
depression, lethargy, blurred vision
...
 CVS= Hypotension or hypertension,
arrhythmias, palpitations, and
respiratory difficulties.
 Hematologic= blood dyscrasi...
The BENZODIAZEPINES
 Instruct to avoid consuming
ALCOHOL while taking the drug.
The BENZODIAZEPINES
 Have available FLUMAZENIL as an
antidote for benzodiazepine
overdose.
5-HT1A Agonists as Anxiolytic
Drugs
 Buspirone
 potent (though non-selective) agonist at 5HT1A-
receptors.
 Lacks anti-...
The BARBITURATES
 These are also anxiolytics and
hypnotics with a greater likelihood of
producing sedation, with increase...
Barbiturates
Non-selective CNS depressants
Sedation and unconsciousness
Bind to the GABA receptor and
enhances activity...
Barbiturates
Non-selective CNS depressants
Sedation and unconsciousness
Bind to the GABA receptor and
enhances activity...
MODE OF ACTION
 Interferes with Na and K transport
 Potentiates GABA action on Cl
ACTIONS
 Depression of CNS
 Respiratory depression
 Enzyme induction
CLASSIFICATION
 ULTRA – SHORT
 Thiopental
 Thiamylal
 Methohexital
 Duration: 30min
 SHORT ACTING
 Hexobarbital
 Pentobarbital
 Secobarbital
 Duration: 2hrs
 INTERMEDIATE ACTING
 Amobarbital
 Butabarbital
 Duration: 3 – 5hra
 LONG ACTING
 Barbital
 Phenobarbital
 Duration: > 6hrs
The BARBITURATES
Pharmacodynamics: The Adverse effects
 CNS= CNS depression, somnolence, vertigo,
lethargy, ataxia, parad...
 CVS= bradycardia, Hypotension and
syncope.
 Respi= serious hypoventilation, respiratory
depression and laryngospasms
 ...
Other Notes
 Benzodiazepines have no analgesic
properties
 Fatality of alcohol and benzodiazepines
 Hypnotics does not ...
Sedative-Hypnotics: Barbiturates
Drug Interactions
 Additive effects:
 ETOH, antihistamines, benzodiazepines,
narcotics,...
Benzodiazepines vs. Barbiturates
Criteria BZ Barb.
Relative Safety High Low
Maximal CNS depression Low High
Respiratory De...
Ion channel that contains the
GABA receptor:
A. sodium
B. calcium
C. chloride
D.potassium
Anxiolytic drug acting through
serotonin receptors:
A.diazepam (Valium)
B. buspirone (BuSpar)
C. triazolam (Halcion)
D. ph...
A comatose patient is brought to the emergency
department with severe respiratory
depression caused by diazepam overdosage...
Short-acting benzodiazepine
A. diazepam (Valium)
B. flurazepam (Dalmane)
C. triazolam (Halcion)
D. buspirone (BuSpar)
Most useful in reversing symptoms
of benzodiazepine overdosage:
A. amphetamine
B. buspirone (BuSpar)
C.flumazenil (Romazic...
Anxiolytic new
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Anxiolytic new

  1. 1. Pharmacology PHARMA BOARD
  2. 2. Anxiety  Fear, apprehension and worry  Accompanied by physical sensations such as anxiety, nausea, chest pain and/or shortness of breath
  3. 3. Neurotransmitters  Excitatory NTs  Key words: sodium, calcium, depolarization  Inhibitory NTs  Key: chloride, GABA, hyperpolarization
  4. 4. Excitatory neurotransmitters  opens Na or Ca channels/ influx depolarization (more positive) nerve impulse  e.g. Norepinephrine, Dopamine, Acetylcholine, Glutamate, Aspartate
  5. 5. Inhibitory neurotransmitters  opens Cl channels hyperpolarization (more negative)  no nerve impulse  e.g. glycine, gamma-aminobutyric acid (GABA)
  6. 6.  1. Panic disorder- recurrent unexpected panic attacks that can occur with agoraphobia in which patients fear places in which escape might be difficult.  2. Specific phobia- intense fear of particular objects or situations (e.g. snakes, heights);most common psychiatric disorder
  7. 7.  3. Social phobia-intense fear of being scrutinized in social or public situations (e.g., giving a speech, speaking in class).  4. Generalized anxiety disorder- intense pervasive worry over virtually every aspect of life
  8. 8.  5. Post-traumatic stress disorder- persistent reexperience of a trauma, efforts to avoid recollecting the trauma, and hyperarousal  6. Obsessive-compulsive disorder- recurrent obsessions and compulsions that cause significant distress and occupy a significant portion of one’s life
  9. 9. Sedatives-Hypnotics  Benzodiazepines  Increase the frequency of GABA-mediated chloride ion channel opening  Barbiturates  Increase the duration of GABA-mediated chloride ion channel opening
  10. 10. Classes of Anxiolytic and Hypnotic drug Benzodiazepines  5-HT1A-receptor agonists  β-adrenoceptor antagonists
  11. 11. Benzodiazepines  Act by binding to a specific regulatory site on the GABA A-receptor  enhances the inhibitory effect of GABA.  Subtypes of the GABA A-receptor exist in different regions of the brain  differ in their sensitivity to benzodiazepines.  Anxiolytic benzodiazepines are agonists at this regulatory site.
  12. 12. Receptor Empty Intra cellular GABA GABA Receptor - CL +++++++ - - - - - NaChannel NaChannel
  13. 13. Intra cellular GABA GABA Receptor - CL + + + + - - - - NaChannel NaChannel - - - -
  14. 14. Use of The Drugs Clinical indications for the use of the anxiolytics, sedatives and hypnotics  1. Prevention of anxiety  2. Formation of sedative state  3. Induction of sleep
  15. 15. ACTIONS  Reduction of anxiety  Sedative – hypnotics  Anticonvulsant  Muscle relaxant
  16. 16. The BENZODIAZEPINES The benzodiazepines are the most frequently used anxiolytic drugs. These agents prevent anxiety states without causing much sedation, with less physical dependence than other agents.
  17. 17. The BENZODIAZEPINES  Long Acting  Intermediate Acting  Short Acting
  18. 18. Long Acting (1-3 days)  Charlie Chaplein Died From Q-fever
  19. 19. Long Acting (1-3 days)  Charlie - Chlorazepate  Chaplein - Chlordiazepoxide  Died - Diazepam  From - Flurazepam  Q-fever - Quazepam
  20. 20. Intermediate  L A T E
  21. 21. Intermediate  L - Lorazepam  A - Alprazolam  T - Temazepam  E - Estazolam
  22. 22. Short Acting  O- Oxazepam  T- Triamzolam
  23. 23.  Uses:  Anxiety- alprazolam, diazepam  Seizures- diazepam, clonazepam, lorazepam  Insomnia- flurazepam, midazolam  Pre-operative sedation- midazolam
  24. 24. The BENZODIAZEPINES Special uses Diazepam (Valium) Status epilepticus Chlordiazepoxide (Librium) Alcohol withdrawal Alprazolam (Xanax) Panic attack
  25. 25. The BENZODIAZEPINES These agents are indicated for the treatment of 1. anxiety disorders 2. alcohol withdrawal 3. hyperexcitability, and agitation 4. pre-operative relief of anxiety and tension and in induction of balanced anesthesia.
  26. 26. The BENZODIAZEPINES Pharmacodynamics: The adverse effects  CNS effects= drowsiness, depression, lethargy, blurred vision  GIT= dry mouth, constipation, nausea, vomiting . sedation,
  27. 27.  CVS= Hypotension or hypertension, arrhythmias, palpitations, and respiratory difficulties.  Hematologic= blood dyscrasias and anemia  GU= urinary retention, hesitancy, loss of libido and sexual functions changes.
  28. 28. The BENZODIAZEPINES  Instruct to avoid consuming ALCOHOL while taking the drug.
  29. 29. The BENZODIAZEPINES  Have available FLUMAZENIL as an antidote for benzodiazepine overdose.
  30. 30. 5-HT1A Agonists as Anxiolytic Drugs  Buspirone  potent (though non-selective) agonist at 5HT1A- receptors.  Lacks anti-seizure and muscle relaxant properties as benzodiazepines  Headache, minimal tolerance and withdrawal  Anxiolytic effects take days or weeks to develop.  Ipsapirone and Gepirone are similar.  Side effects include dizziness, nausea, headache, but not sedation or loss of coordination
  31. 31. The BARBITURATES  These are also anxiolytics and hypnotics with a greater likelihood of producing sedation, with increase risk of addiction and dependence.
  32. 32. Barbiturates Non-selective CNS depressants Sedation and unconsciousness Bind to the GABA receptor and enhances activity potent inducers of hepatic drug- metabolising enzymes Tolerance and dependence occur.
  33. 33. Barbiturates Non-selective CNS depressants Sedation and unconsciousness Bind to the GABA receptor and enhances activity potent inducers of hepatic drug- metabolising enzymes Tolerance and dependence occur.
  34. 34. MODE OF ACTION  Interferes with Na and K transport  Potentiates GABA action on Cl
  35. 35. ACTIONS  Depression of CNS  Respiratory depression  Enzyme induction
  36. 36. CLASSIFICATION  ULTRA – SHORT  Thiopental  Thiamylal  Methohexital  Duration: 30min
  37. 37.  SHORT ACTING  Hexobarbital  Pentobarbital  Secobarbital  Duration: 2hrs
  38. 38.  INTERMEDIATE ACTING  Amobarbital  Butabarbital  Duration: 3 – 5hra
  39. 39.  LONG ACTING  Barbital  Phenobarbital  Duration: > 6hrs
  40. 40. The BARBITURATES Pharmacodynamics: The Adverse effects  CNS= CNS depression, somnolence, vertigo, lethargy, ataxia, paradoxical excitement, anxiety and hallucinations.  GIT= nausea, vomiting, constipation/diarrhea and epigastric pain
  41. 41.  CVS= bradycardia, Hypotension and syncope.  Respi= serious hypoventilation, respiratory depression and laryngospasms  Others= hypersensitivity and Stevens- Johnson syndrome.
  42. 42. Other Notes  Benzodiazepines have no analgesic properties  Fatality of alcohol and benzodiazepines  Hypnotics does not induce REM so less restful than normal sleep  Longer acting drugs are easier to dose so effective in alcohol withdrawal
  43. 43. Sedative-Hypnotics: Barbiturates Drug Interactions  Additive effects:  ETOH, antihistamines, benzodiazepines, narcotics, tranquilizers  Inhibited metabolism:  MAOIs will prolong effects of barbiturates  Increased metabolism:  Reduces anticoagulant response, leading to possible clot formation
  44. 44. Benzodiazepines vs. Barbiturates Criteria BZ Barb. Relative Safety High Low Maximal CNS depression Low High Respiratory Depression Low High Suicide Potential Low High Abuse Potential Low High Antagonist Available? Yes No
  45. 45. Ion channel that contains the GABA receptor: A. sodium B. calcium C. chloride D.potassium
  46. 46. Anxiolytic drug acting through serotonin receptors: A.diazepam (Valium) B. buspirone (BuSpar) C. triazolam (Halcion) D. phenobarbital
  47. 47. A comatose patient is brought to the emergency department with severe respiratory depression caused by diazepam overdosage. Reasonable intervention at this point include: A. administer naloxone (Narcan) to block the drug's effect at the receptor B. provide supportive therapy until the drug effect wears off. C. administer flumazenil D. B & C
  48. 48. Short-acting benzodiazepine A. diazepam (Valium) B. flurazepam (Dalmane) C. triazolam (Halcion) D. buspirone (BuSpar)
  49. 49. Most useful in reversing symptoms of benzodiazepine overdosage: A. amphetamine B. buspirone (BuSpar) C.flumazenil (Romazicon) D. naltrexone (ReVia)
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