CNS Anticonvulsants

Question 1

Anti-seizure meds with MOA:
Decreased axonal conduction by preventing Na+ influx through fast
Na channels:

Answer 1

carbamazepine, phenytoin

Question 2

Anti-seizure meds with MOA:
Increased inhibitory tone by facilitation of GABA-mediated hyperpo-
larization:

Answer 2

barbiturates, benzodiazepines

Question 3

Anti-seizure meds with MOA:
Decreased excitatory effects of glutamic acid
(blocks AMPA receptors)

Answer 3

lamotrigine, topiramate

Question 4

Anti-seizure meds with MOA:
Decreased excitatory effects of glutamic acid
(blocks NMDA receptors)

Answer 4

felbamate

Question 5

Anti-seizure meds with MOA:

Decreased presynaptic Ca2+ influx through type-T channels in thalamic neurons:

Answer 5

ethosuximide and valproic acid

Question 6

Tx for General—absence seizures

MOA: blockade of T-type Ca2+ channels in thalamic neurons

Answer 6

Ethosuximide

Question 7

Tx for Status epilepticus

Answer 7

Lorazepam, diazepam, phenytoin, or fosphenytoin*

Question 8

Tx for Partial—simple or complex and General—tonic-clonic

Answer 8

Valproic acid, phenytoin, carbamazepine, lamotrigine

Question 9

Blocks axonal Na+ channels in their inactivated state
– Prevents seizure propagation
– Uses: seizure states

Variable absorption
o Nonlinear kinetics
o Induction of cytochrome P450s
o Zero-order kinetic of elimination

Side effects:
o CNS depression
o Gingival hyperplasia
o Hirsutism
o Osteomalacia (↓ vitamin D)
o Megaloblastic anemia (↓ folate)
o Aplastic anemia (check hematology lab results)
– Teratogenicity: cleft lip and palate

Answer 9

Phenytoin

Question 10

Mechanism identical to phenytoin
– Uses:
o Seizure states
o DOC for trigeminal neuralgia
o Bipolar disorder

Pharmacokinetics: induces cytochrome P450, including its own metabolism
– Side effects:
o CNS depression
o Osteomalacia
o Megaloblastic anemia
o Aplastic anemia
o Exfoliative dermatitis
o ↑ ADH secretion (dilutional hyponatremia)
– Teratogenicity: cleft lip and palate; spina bifida

Answer 10

Carbamazepine

Question 11

Mechanism:
o Similar to phenytoin
o But also inhibition of GABA transaminase
o Blockade of T-type Ca2+ channels
– Uses:
o Seizure states
o Mania of bipolar disorders
o Migraine prophylaxis
– Pharmacokinetics: inhibits cytochrome P450s

Answer 11

Valproic acid

Question 12

Side effects:
o Hepatotoxicity (from toxic metabolite)
o Thrombocytopenia
o Pancreatitis
o Alopecia
– Teratogenicity: spina bifida

Answer 12

Valproic acid

Question 13

– Blocks Na+ channels and glutamate receptors
– Used in various seizures
– Side effects: Stevens-Johnson syndrome

Answer 13

Lamotrigine

Question 14

– Blocks Na+ channels and glutamate receptors and enhances GABA
activity
– Used in focal seizures in adults and children > age 2; also used in migraine prophylaxis
– Side effects: weight loss

Answer 14

Topiramate

Question 15

– Block Na+ channels and glutamate receptors
– Used in seizure states (often adjunct therapy)
– Side effects: Aplastic anemia

Answer 15

Felbamate

Question 16

– May affect calcium channels and neurotransmitter release,
GABA effects
– Used in seizure states, neuropathic pain (such as postherpetic neuralgia)

Answer 16

Gabapentin

Question 17

• ↓ efficacy of oral contraceptives via induction of cytochrome P450

Answer 17

Carbamazepine, Phenytoin, Phenobarbital

Question 18

Least potent inhaled anethestics

Answer 18

Nitrous oxide

Question 19

Most potent inhaled anethestics

Answer 19

Sevoflurane and

Desflurane

Question 20

IV Anesthetics
– Benzodiazepine used for:
o Preoperative sedation
o Anterograde amnesia o Induction
o Outpatient surgery
– Depresses respiratory function

Answer 20

Midazolam

Question 21

IV Anesthetics
Used for induction and maintenance of anesthesia
– Antiemetic
– CNS and cardiac depressant

Answer 21

Propofol

Question 22

IV Anesthetics
– Opiate used for induction and maintenance of anesthesia
– Depresses respiratory function

Answer 22

Fentanyl

Question 23

IV Anesthetics
 Dissociative anesthetic
– NMDA-receptor antagonist
– Induction of anesthesia
– Emergent delirium, hallucinations
– Cardiovascular stimulation
– ↑intracranial pressure

Answer 23

Ketamine

Question 24

LOCAL ANESTHETICS

Esters

Answer 24

Have one “I” in them
procaine, cocaine, benzocaine
and can cause allergies

Question 25

LOCAL ANESTHETICS | Amides

Answer 25

Have two "I"s in them | lidocaine, bupivacaine, mepivacaine

Question 26

Antidote that acts directly on skeletal muscle to decrease contractility by blocking Ca2+ release from the sarcoplasmic reticulum.

Answer 26

Dantrolene

Question 27

Nondepolarizing (competitive)

Answer 27

Nicotinic antagonists Rocuronium is the prototype – Reversible with AChE inhibitors

Question 28

Nondepolarizing (competitive) | (rapid recovery, safe in hepatic or renal impairment, spontaneous inactivation to laudanosine

Answer 28

Atracurium

Question 29

Depolarizing (noncompetitive)

Answer 29

Nicotinic agonist | – Specific drug: succinylcholine

Question 30

Drug associated with Malignant Hyperthermia

Answer 30

Succinylcholine

Question 31

Analgesia: ↑ pain tolerance and ↓ perception and reaction to pain • Sedation Respiratory depression: ↓ response to ↑ pCO2

Answer 31

Morphine

Question 32

Antidote to Opioid OD

Answer 32

Naloxone

Question 33

Smooth muscle: longitudinal relaxes; circular constricts – GI: * peristalsis, constipation, cramping – GU: urinary retention, urgency to void – Biliary: + pressure – Pupils: miosis

Answer 33

Symptoms from Opiod OD

Question 34

Nausea and vomiting: stimulation of the chemoreceptor trigger zone (CTZ) in the area postrema • Increased histamine release • Pharmacokinetics: glucuronidation; morphine-6-glucuronide is highly active; caution in renal dysfunction

Answer 34

Morphine

Question 35

Opioids and Analgesics | with Full agonist action

Answer 35

Meperidine Methadone Codeine

Question 36

Opioids and Analgesics | with Partial agonist action

Answer 36

Buprenorphine

Question 37

Opioids and Analgesics | Mixed agonist- antagonists

Answer 37

Nalbuphine, pentazocine

Question 38

Full Agonist with: - antimuscarinic action - No miosis - Tachycardia No spasm GI/GU/gallbladder • Metabolized by cytochrome P450 to normeperidine, a serotonin reuptake inhibitor; normeperidine may cause serotonin syndrome and seizures

Answer 38

Meperidine

Question 39

Used in maintenance of opiate addict

Answer 39

Methadone

Question 40

Cough suppressant • Analgesia • Used in combination with NSAIDs

Answer 40

Codeine

Question 41

Partial Agonists capable of Precipitation of Withdrawal

Answer 41

Buprenorphine

Question 42

Mixed agonist- antagonists with action as a κ-agonist spinal analgesia dysphoria

Answer 42

Nalbuphine

Question 43

μ antagonist that can cause precipitation of withdrawal

Answer 43

pentazocine

Question 44

IV, reversal for respiratory depression

Answer 44

Naloxone

Question 45

PO, ↓ craving for alcohol and used in opiate addiction

Answer 45

Naltrexone

Question 46

Treatment of opioid-induced constipation (does not cross BBB and won’t precipitate withdrawal)

Answer 46

Methylnaltrexone

Question 47

combination of buprenorphine and naloxone used for opioid addiction to prevent abuse

Answer 47

Suboxone

Question 48

Acute toxicity: classic triad o Pinpoint pupils o Respiratory depression o Coma

Answer 48

Opioid S/E

Question 49

``` Withdrawal: o Yawning o Lacrimation, rhinorrhea, salivation o Anxiety, sweating, goose bumps o Muscle cramps, spasms, CNS-originating pain ```

Answer 49

Opioid Abuse

Question 50

Opioid used for diarrhea

Answer 50

Loperamide

Question 51

Opioid used for cough

Answer 51

Dextromethorphan