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Pharm - General Principles > CNS Anticonvulsants > Flashcards

CNS Anticonvulsants Flashcards

1
Q

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

A

carbamazepine, phenytoin

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2
Q

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

A

barbiturates, benzodiazepines

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3
Q

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

A

lamotrigine, topiramate

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4
Q

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

A

felbamate

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5
Q

Anti-seizure meds with MOA:

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

A

ethosuximide and valproic acid

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6
Q

Tx for General—absence seizures

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

A

Ethosuximide

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7
Q

Tx for Status epilepticus

A

Lorazepam, diazepam, phenytoin, or fosphenytoin*

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8
Q

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

A

Valproic acid, phenytoin, carbamazepine, lamotrigine

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9
Q

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
A

Phenytoin

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10
Q 
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

A

Carbamazepine

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11
Q 
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
A

Valproic acid

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12
Q 
Side effects:
o Hepatotoxicity (from toxic metabolite)
o Thrombocytopenia
o Pancreatitis
o Alopecia
– Teratogenicity: spina bifida
A

Valproic acid

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13
Q

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

A

Lamotrigine

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14
Q

– 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

A

Topiramate

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15
Q

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

A

Felbamate

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16
Q

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

A

Gabapentin

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17
Q

• ↓ efficacy of oral contraceptives via induction of cytochrome P450

A

Carbamazepine, Phenytoin, Phenobarbital

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18
Q

Least potent inhaled anethestics

A

Nitrous oxide

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19
Q

Most potent inhaled anethestics

A

Sevoflurane and

Desflurane

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20
Q 
IV Anesthetics
– Benzodiazepine used for:
o Preoperative sedation
o Anterograde amnesia o Induction
o Outpatient surgery
– Depresses respiratory function
A

Midazolam

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21
Q

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

A

Propofol

22
Q

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

A

Fentanyl

23
Q 
IV Anesthetics
 Dissociative anesthetic
– NMDA-receptor antagonist
– Induction of anesthesia
– Emergent delirium, hallucinations
– Cardiovascular stimulation
– ↑intracranial pressure
A

Ketamine

24
Q

LOCAL ANESTHETICS

Esters

A

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

25
Q

LOCAL ANESTHETICS

Amides

A

Have two “I”s in them

lidocaine, bupivacaine, mepivacaine

26
Q

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

A

Dantrolene

27
Q

Nondepolarizing (competitive)

A

Nicotinic antagonists
Rocuronium is the prototype
– Reversible with AChE inhibitors

28
Q

Nondepolarizing (competitive)

(rapid recovery, safe in hepatic or renal impairment, spontaneous inactivation to laudanosine

A

Atracurium

29
Q

Depolarizing (noncompetitive)

A

Nicotinic agonist

– Specific drug: succinylcholine

30
Q

Drug associated with Malignant Hyperthermia

A

Succinylcholine

31
Q

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

A

Morphine

32
Q

Antidote to Opioid OD

A

Naloxone

33
Q

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

A

Symptoms from Opiod OD

34
Q

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

A

Morphine

35
Q

Opioids and Analgesics

with Full agonist action

A

Meperidine Methadone Codeine

36
Q

Opioids and Analgesics

with Partial agonist action

A

Buprenorphine

37
Q

Opioids and Analgesics

Mixed agonist- antagonists

A

Nalbuphine, pentazocine

38
Q

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

A

Meperidine

39
Q

Used in maintenance of opiate addict

A

Methadone

40
Q

Cough suppressant
• Analgesia
• Used in combination with NSAIDs

A

Codeine

41
Q

Partial Agonists capable of Precipitation of Withdrawal

A

Buprenorphine

42
Q

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

A

Nalbuphine

43
Q

μ antagonist that can cause precipitation of withdrawal

A

pentazocine

44
Q

IV, reversal for respiratory depression

A

Naloxone

45
Q

PO, ↓ craving for alcohol and used in opiate addiction

A

Naltrexone

46
Q

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

A

Methylnaltrexone

47
Q

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

A

Suboxone

48
Q

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

A

Opioid S/E

49
Q 
Withdrawal: 
o Yawning
o Lacrimation, rhinorrhea, salivation
o Anxiety, sweating, goose bumps
o Muscle cramps, spasms, CNS-originating pain
A

Opioid Abuse

50
Q

Opioid used for diarrhea

A

Loperamide

51
Q

Opioid used for cough

A

Dextromethorphan

Pharm - General Principles (11 decks)

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