SEDATIVE-HYPNOTIC-ALCOHOLDRUGS

Question 1

site of action of benzodiazepines, barbiturates
and other related drugs (i.e. Zolpidem, Zaleplon, Eszopiclone)

Answer 1

GABA-A Receptor

This is different from GABA-B receptor, of which the agonist is the drug Baclofen).

Question 2

WHAT ARE THE 5 PRINCIPLE PHARMACOLOGIC EFFECTS
OF YOUR BENZODIAZEPINES?

Answer 2

1. Anxiolysis
2. Sedation and hypnosis
3. Anticonvulsant actions
4. Spinal cord mediated skeletal muscle relaxation
5. Anterograde amnesia

This effect is very specific to benzodiazepines

Question 3

Preferred Benzo as anticonvulsant maintenance?

Answer 3

Clonazepan

Question 4

Preferred Benzo for status epilepticus?

Answer 4

Lorazepam, Diazepam

Question 5

Preferred Benzo for Skeletal muscle relaxation
(e.g. cerebral palsy)

Answer 5

DIAZEPAM

Question 6

Preferred Benzo for Panic Disorders, Phobia

Answer 6

Alprazolam, Clonazepam

Question 7

Preferred Benzo for anesthesia induction?

Answer 7

Midazolam, Diazepam, Lorazepam

Question 8

Preferred Benzo for Bipolar Disorder?

Answer 8

Clonazepam

Question 9

Preferred Benzo for Alcohol Withdrawal?

Answer 9

Chlordiazepoxide

Question 10

Treatment for Benzo overdose?

Answer 10

FLUMAZENIL (BZD RECEPTOR ANTAGONIST)

Question 11

FLUMAZENIL MOA?

Answer 11

Competitive Antagonist at benzodiazepine sites on
GABA-A receptor

Question 12

Short Acting Benzos?

Answer 12

Triazolam, Oxazepam,
Midazolam, Brotizolam, Etizolam

Question 13

Long Acting Benzos

Answer 13

Diazepam, Chlordiazeopoxide,
Chlorazepate, Flurazepam,
Quazepam, Flunitrazepam
* Note: Flunitrazepam: ‘date rape dr

Question 14

Intermediate Acting benzos

Answer 14

Lorazepam, Alprazolam,
Estazolam, Clonazepam,
Lormetazepam, Nitrazepam,
Temazepam
Note: Lorazepam can be used for status
epilepticus and Clonazepam +
Alprazolam can be used in panic attacks
and anxiety disorder

Question 15

BARBITURATES MOA?

Answer 15

Bind to GABA-A receptor sites (distinct from
benzodiazepines); allosterically modulates the receptor to
increase duration of chloride channel opening; block
glutamate neurotransmission via voltage-gated calcium
channels

Question 16

Barbiturates is contraindicated in?

Answer 16

Porphyria

Question 17

What barbiturate is used for Seizures, status epilepticus,
hyperbilirubinemia (Gilbert or Type II
Crigler-Najar syndrome), drug of choice
for neonatal seizures

Answer 17

(pheno-baby-tal) Phenobarbital

Question 18

What barbiturates is used for essential tremors?

Answer 18

PRIMIDONE

Question 19

What barbiturates is used for Induction and maintenance of
anesthesia, pre-op sedation, emergency
management of seizures, intracranial
pressure
Note: rapidly redistributed to skeletal muscle &
adipose; very highly lipid soluble

Answer 19

Thiopental

Question 20

MOA of ZOLPIDEM, ZALEPLON, ESZOPICLONE

Answer 20

Bind selectively to a subgroup of GABA-A receptors,
acting like benzodiazepines; interact with GABA-A
receptors with alpha-1 subunit

Question 21

Reversing Agent of Z drugs?

Answer 21

FLUMAZENIL

Question 22

BUSPIRONE MOA?

Answer 22

5HT1A Partial agonist; also D2 agonist
ANXIOLYTICS

Question 23

Methanol creates ??? which causes visual disturbance, coma, seizures

Answer 23

FORMATE

Question 24

Ethylene glycol (antifreeze): creates toxic ??? and
??? , which causes kidney damage and severe acidosis

Answer 24

Ethylene glycol (antifreeze): creates toxic aldehydes and
oxalate, which causes kidney damage and severe acidosis

Question 25

“BLACKOUTS” (i.e. periods of memory loss that occurs with high levels of
alcohol intoxication) are a result of inhibition of?

Answer 25

“BLACKOUTS” (i.e. periods of memory loss that occurs with high levels of
alcohol intoxication) are a result of inhibition of NMDA activation

Question 26

What drugs can cause disulfiram reaction?

Answer 26

“Clara took the Pre-Medical Test in the PM”

Chlorpropamide, CEFO (PERAZONE, MANDOLE, TETAN)

Procarbazine
Metronidazole

Question 27

Fetal Alcohol Syndrome?

Answer 27

mental
retardation, microcephaly,
underdevelopment of midface region

Question 28

Syndrome resulting from
chronic alcohol excess and
thiamine deficiency

Answer 28

Wernicke-Korsakoff
Syndrome

Question 29

Triad of Wernicke’s
encephalopathy

Answer 29

confusion,
ophthalmoplegia, ataxia

Question 30

Triad of Korsakoff Syndrome:

Answer 30

irreversible memory loss,
confabulation, personality
change

Question 31

Treatment of Wernicke Korsakoff Syn?

Answer 31

Thiamine and Glucose, give thiamine first

Question 32

Alcohol withdrawal aka?

Answer 32

Delirium Tremens

Question 33

Features of Delirium Tremens?

Answer 33

Altered mental
status,
hallucinations,
seizures, tremors

Question 34

Tx of Delirium Tremens?

Answer 34

Benzodiazepines
(chlordiazepoxide,
lorazepam)

Question 35

Disulfiram MOA?

Answer 35

• Deterrent
• Inhibits ALDH with
  resulting ↑
  acetaldehyde after
  drinking.
• Causes hangover
  symptoms = patients
  avoid alcohol

Question 36

MOA Naltrexone

Answer 36

μ-opioid receptor
antagonist. ↓
drinking through
* ↓ feelings of reward
with
* alcohol or ↓ craving.

Question 37

MOA Acamprosate?

Answer 37

• Blocks
  hyperglutamergic
  state of alcoholic
  brain causing
  decreased feeling of
  “need” for alcohol

Question 38

CLinical features of Methanol Poisoning?

Answer 38

Visual dysfunction (gin bulag), gastrointestinal distress,
shortness of breath, loss of consciousness, coma
● accumulation of formaldehyde and formic acid causes severe
acidosis, retinal damage, and blindness

Question 39

Clinical Features of Ethylene Glycol Poisoning

Answer 39

Severe acidosis and renal damage

Question 40

Treatment of Methanol or Ethylene Glycol Poisoning?

Answer 40

ETHANOL – no longer first line!
● acts as a preferred substrate for alcohol dehydrogenase
● competitively inhibits the oxidation of methanol
FOMEPIZOLE - inhibitor of alcohol dehydrogenase, now preferred over ethanol