Opiods, Antiepileptics, Anaesthetics

Question 1

What are some examples of opioid drugs?

Answer 1

Morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan, diphenoxylate

Question 2

Mechanism of opioids?

Answer 2

Agonists at opioid receptors to modulate synaptic transmission.

Question 3

What drugs correspond to the following receptors?
mu
delta
kappa

Answer 3

mu = morphine
delta = enkephalin
kappa = dynorphin

Question 4

What channels do opiods act on?

Answer 4

open K+ channels, close Ca2+ channels

Question 5

Which NTs are prevented from release by opioid activity?

Answer 5

ACh, NE, 5-HT, glutamate, substance P

Question 6

Which opioid is indicated for cough suppression?

Answer 6

dextromethorphan

Question 7

Which opioids are indicated for diarrhea?

Answer 7

loperamide and diphenoxylate

Question 8

What analgesic class can be used to treat acute pulmonary edema?

Answer 8

opioids

Question 9

What are two toxicities of opiods that patients do not develop tolerance to?

Answer 9

miosis and constipation

Question 10

How can you treat toxicity of opioids?

Answer 10

opioid receptor antagonists: naloxone or naltrexone

Question 11

What drug is a partial agonist of mu and kappa- receptors?

Answer 11

Butorphanol

Question 12

What is the advantage of using Butorphanol over other opioids?

Answer 12

It causes less respiratory depression than full agonists

Question 13

What are two toxicities of Butorphanol?

Answer 13

1. Because it’s a partial agonist, it can cause withdrawal if giving concomitantly with full agonists
2. Overdose not easily reversed with nalaxone

Question 14

What is tramadol?

Answer 14

A very weak opioid agonist; it also inhibits serotonin and NE reuptake – “tram it all” with tramadol)

Question 15

What is butorphanol indicated for?

Answer 15

Severe pain such as migraines and labor

Question 16

What is tramadol indicated for?

Answer 16

chronic pain

Question 17

What are toxicities of tramadol?

Answer 17

1. similar to opiods
2. decreases seizure threshold
3. serotonin syndrome

Question 18

What is the mechanism of Ethosuximide?

Answer 18

Blocks thalamic T-type Ca2+ channels

Question 19

What are the side effects of Ethosuximide?

Answer 19

EFGHIJ: Ethosuximide causes fatigue, GI distress, Headache, Itching (urticaria), and Stevens-Johnson syndrome

Question 20

What is ethosuximide used for?

Answer 20

absence seizures

Question 21

What kind of seizures are benzodiazapenes used for?

Answer 21

1. Status epilipticus

2. Eclampsia seizures (1st line is MgSO4)

Question 22

What is the mechanism of benzos?

Answer 22

Increases GABA(a) action

Question 23

What are side effects of benzos?

Answer 23

Sedation, tolerance, dependence, respiratory depression

Question 24

What are three indications for phenytoin?

Answer 24

1. Partial seizures (simple and complex)
2. tonic clonic (1st line)
3. status epilepticus prevention

Question 25

Side effects of phenytoin:

Answer 25

Eyes: nastagmus, diplopia Mouth: gingival hyperplasia Nerves: ataxia, sedation, peripheral neuropathy Metabolic: induction of P450 Blood: megaloblastic anemia (inhibits intestinal conjugase); Lymph: lymphadenopathy Bone: osteopenia Skin: Stevens Johnson Syndrome Developmental: fetal hydantoin syndrome (teratogenesis)

Question 26

What are the indications for carbamazepine?

Answer 26

1st line for partial (simple and complex) and tonic-clonic

Question 27

What is the mechanism of action of carbamazepine?

Answer 27

Na+ channel inactivation

Question 28

Side effects of carbamazepine:

Answer 28

Eyes: diplopia Nerves: ataxia Metabolic: induction of P450, liver toxicity Blood: dyscrasias (agranulocytosis, aplastic anemia) Skin: Stevens-Johnson Development: Teratogenesis

Question 29

What is the mechanism of action of Valproic acid?

Answer 29

Na+ channel inactivation, increased GABA concentration by inhibiting GABA transaminase

Question 30

What are some toxicities of Valproic acid?

Answer 30

GI, distress, fatal hepatotoxicity (rare, measure LFTs), neural tube defects (spina bifida), tremor, weight gain, contraindicated in pregnancy

Question 31

What is valproic acid for?

Answer 31

all seizures except status epilepticus, myoclonic seizures, bipolar disorder

Question 32

What three drugs are used primarily for partial seizures?

Answer 32

Gabapentin, Tiaginbine, Vigabatrin

Question 33

Primary side effects of gabapentin?

Answer 33

Sedation, ataxia

Question 34

Mechanism of gabapentin?

Answer 34

high voltage-activated Ca2+ channels despite designation as GABA analog

Question 35

What drug can be used for migraine prophylaxis?

Answer 35

gabapentin

Question 36

Which antiepileptics can be used for bipolar d/o?

Answer 36

Valproic acid and gabapentin

Question 37

Which antiseizure drug is marketed for postherpetic neuralgia?

Answer 37

gabapentin

Question 38

Which antiseizure drug is marketed as first line for trigeminal neuralgia?

Answer 38

carbamazapine

Question 39

Phenobarbital mechanism and indications

Answer 39

Increases GABA(a) (like phenytoin) and is used to treat partial and tonic-clonic seizures

Question 40

What are the mechanism and indications for topiramate?

Answer 40

Blacks Na+ channels, increases GABA action | Indicated for partial and tonic-clonic

Question 41

Indications and mechanism for lamotrigine

Answer 41

partial, tonic clonic; blocks voltage-gated Na+ channels

Question 42

Toxicity of lamotrigine

Answer 42

Stephens-Johnson (must be titrated slowly)

Question 43

Mechanism and indications for levetiracetam

Answer 43

unknown (may modulate GABA and Glu release); partial and TC

Question 44

Indications and mechanisms for Tiagabine and Vigabatrin

Answer 44

both indicated for partial seizures; increase GABA by inhibiting uptake (Tiagabine) and transaminase (Vigabatrin)

Question 45

What are some barbituates?

Answer 45

Phenobarbital, penorbital, thiopental, secorbarbital

Question 46

What do barbituates work?

Answer 46

Facilitate GABAa action by increasing duration of Cl- channel opening--> decrease neuron firing

Question 47

Clinical uses for barbituates

Answer 47

sedative for: anxiety, seizures, insomnia, induction of anesthesia

Question 48

What drug is used as a sedative for induction of anesthesia? What class of drug is this?

Answer 48

Thiopental; barbituate

Question 49

Toxicities of barbituates

Answer 49

Respiratory and cardiovascular depression (can be fatal) CNS depression (can be exacerbated by EtOH use) Dependence Drug interactions (induces P450)

Question 50

How do you treat a barbituate overdose?

Answer 50

Supportive: assist respiration and maintain BP

Question 51

What are some examples of Benzodiazepines?

Answer 51

Diazepam, lorazempam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide, alprazolam