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Pharmacology II > Drugs for Test 1 > Flashcards

Drugs for Test 1 Flashcards

1
Q

What are the first line DOC based on seizure type for partial seizures?

A 
Carbamzepine
Phenytoin
Lamotrigine
Oxcarbazepine
Topiramate
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2
Q

What are the second line DOC based on seizure type for partial seizures?

A 
Gabapentin
Levetiracetam
Phenobarbital
Pregabalin
Primidone
Tiagabine
Valproic acid
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3
Q

What are the first line DOC based on seizure type for absence seizures?

A

Ethosuximide
Lamotrigine
Valproic acid

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4
Q

What are the first line DOC based on seizure type for myoclonic and atonic seizures?

A

Valproic acid

Lamotrigine

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5
Q

What are the first line DOC based on seizure type for tonic-clonic seizures?

A

Valproic acid
Carbamazepine
Oxcarbazepine
Lamotrigine

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6
Q

Phenytoin (Dilantin) MOA and Indications

A

Blocks voltage gated Na+ channels reducin the propogation of abnormal impulses in the brain.
Indications- simple and complex partial sz, generalized tonic-clonic sz, and status epilepticus caused by recurrent tonic-clonic sz.

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7
Q

Phenytoin Pharmakokinetics and administration considerations

A

Metabolized by P450 system
Potent non-specific inducer of many drug metabolizing enzymes
Highly protein bound
Nonlinear kinetics
Requires dosing therapeutic monitoring
Enteral feeding reduces oral absorption, oral suspension shake vigoriously.
IV formulation can cause pain, phlebitis, and extravasation.
No IM injection

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8
Q

Phenytoin anti arrhythmia and drug interactions

A

Dont stop abruptly
Inducers- carbamazepine, OCP, doxyclycline, quinidine, cyclosporin, methadone, levodopa
Inhibitors- chloramphenicol, CIMETIDINE sulfonamide, and ISONIAZID

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9
Q

Phenytoin ADRs

A

Dose related- nystagmus, ataxia, drowsiness, cognitive impairment
Non-dose related- GINGIVAL HYPERPLASIA, hirsutism, acne, rash, hepatotoxicity
Teratogenic- Fetal hydantoin syndrome (cleft lip and palate, congenital heart disease, slowed growth and mental deficiency)

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10
Q

Carbamazepine (Tegretol) MOA and indications

A

Blocks Na+ channels

Indications- first line tx of simple partial, complex partial, and generalized tonic-clonic

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11
Q

Carbamazepine (Tegretol) Pharmakokinetics

A

Monitoring through autoinduction (first 20-30 days of tx, autoinduction is dose dependent, after complete, steady state concentrations are achieved after 3 days)
Potent non-specidic inducer of many drugs and transporters

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12
Q

Carbamazepine (Tegretol) ADRs

A

Dose related- vertigo, ataxia, diplopia, drowsiness, nausea
CNS side effects- HA, paraesthesis, confusion, psychosis
Non-specific- SIADH, leukopenia, thrombocytopenia, stevens johnson syndrome.

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13
Q

Phenobarbital (Luminal) MOA, indications, and side effects

A

MOA unknown
Indications- generalized tonic clonic, partial sz, neonatal sz, febrile sz,
Side effects- sedation, irritability, slowed thinking, ataxia, hyperactivity, and rash

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14
Q

Phenobarbital (Luminal) pharmacokinetics

A

Extremely long 1/2 life (96 hours)
Time to steady state is 20-30 days
Metabolized by P450 system

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15
Q

Primidone (mysoline) MOA and indication

A

Structurally related to phenobarbita l
Efficacy from metabolites (phenobarbital- tonic clonic sz and simple partial sz, and pehnyethylmalonamide- complex partial sz)
Well absorbed orally; poor protein binding, same ADRs as phenobarbital
Indications- alternative choice in partial sz and tonic-clonic sz

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16
Q

Valproic acid (Depakene) & Sodium Valproate (Depakote) MOA and indication

A

Completely absorbed
Saturable protein binding
Hepatic metabolism but DOESN’T induce P450
Inhibits metabolism of phenobarbital, carbamazepine, ethosuximide

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17
Q

What drugs does Valproic acid (Depakene) inhibit the metabolism?

A

Phenobarbital, carbamazepine, ethosuximide.

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18
Q

Valproic acid side effects

A

Dose related- N/V, Abd pain, diarrhea, sedation, tremor, unsteadiness
Non-dose related- acute hepatic failure, acute pancreatitis.

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19
Q

Ethosuximide (Zarontin) MOA and indication

A

MOA- inhibits calcium channels.

Indication- DOC for absence seizures.

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20
Q

Ethosuximide (Zarontin) pharmacokinetics and side effects

A

Absorbed orally; not protein bound; metabolized by but not inducer of P450
Side effects dose related- GI, lethargy, HA, dizziness, anxiety

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21
Q

What are the second generations anti-epileptic drugs?

A 
Gabapentin (neurontin)
Oxcarbamazepine (Trileptal)
Tiagapine (Gabitril)
Felbamate (Felbatol)
Lamotrigine (Lamictal)
Zonisamide (Zonegran)
Levetiracetam (Keppra)
Pregabalin (Lyrica)
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22
Q

Oxcarbamazepine (trileptal) MOA and indication

A

Active metabolite blocks Na+ channels
Indication- partial sz with or w/out secondary generalization
Analogue of cabamazepine w/ fewer side effects than cabamazepine and phenytoin

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23
Q

Oxcarbamazepine (trileptal) Side effects

A

Dizziness, ataxia, fatigue, GI, hyponatremia, rash
30% reactivity for rash with CBZ
No PK monitoring; no autoinduction

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24
Q

Gabapentin (Neurotin) MOA and indication

A

Analog of GABA; MOA unknown

Indication- adjunct to partial and GTC sz, tx of peripheral neuropathy.

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25
Q

Gabapentin (Neurotin) favorable pharmacokinetic profile

A

Dose-dependent oral absorption
Not protein bound
Excreted unchanged via kidneys
No serum level monitoring

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26
Q

Gabapentin (Neurotin) Side effects

A

Somnolence, dizziness, ataxia, nystagmus

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27
Q

Tiagabine (Gabitril) MOA and Indication

A

Competitive inhibitor of GABA transporter in neurons and glia (inhibitors re-uptake)
Indication- adjunctive tx of partial sz
TAKE WITH FOOD

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28
Q

Tiagabine (Gabitril) pharmacokinetics and side effects

A

Quickly and completely absorbed
Increased clearance in peds, with enzyme inducers
Serum concentrations unnecessary
Side effects- Dose related: dizziness, fatigue, nervousness, difficulty concentrating

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29
Q

Lamotrigine (lamictal) MOA and indication

A

Blocks Na+ and Ca++ channels
Adjunctive in children and mono therapy in adults
Indications- GTC, partial seizures, absence

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30
Q

Lamotrigine (lamictal) adverse side effects

A

Rash (10%), confusion, depression, N/V, diplopia, severe idiosyncratic (skin, blood)
Slow taper essential, initial dose dependent on other meds

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31
Q

Topiramate (Topamax) MOA and indication

A

Blocks Na+ channels and binds GABA thus opening Cl- channels

Indication- tx for partial and generalized sz in pediatrics and adults.

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32
Q

Topiramate (Topamax) pharmacokinetics and adverse effects

A 
70% renal elimination
1st order kinetics
Clearance increased w/ enzyme inhibitors
AE- dose related- drowsiness, parasthesias, psychomotor slowing, weight loss, renal calculi
NOTE- Maintain adequate fluid levels
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33
Q

Felbamate (felbtol) MOA and indication

A

Blocks Na+ channels, competes for NMDA receptor, prevents AMPA receptor stimulation, blocks Ca++ channels
Indication- partial sz and lennox-gastaut syndrome
Use restricted to refractory Lennox-Gastaut syndrome (active metabolism covalently binds liver, bone marrow proteins, and DNA resulting in aplastic anemia and liver failure.

34
Q

Felbamate (felbtol) Side effects

A

Dose related- anorexia, N/V, insomnia, HA

Non-dose related- aplastic anemia, hepatic failure

35
Q

Levetiracetam (Keppra) MOA and indication

A

MOA unknown
Indication- tx of generalized sz
Adjust dose in renal insufficiency

36
Q

Levetiracetam (Keppra) favorable PK profile and Side effects

A

Almost completely absorbed
Metabolism NOT dependent on the P450 system
Minimal protein binding
MInimal drug interactions
Side effects- sedation, behavioral abnormalities

37
Q

Zonisamide (Zonegran) MOA and Indication

A

Sulfonamide derivative: blocks Na+ and Ca++ channels and enhances GABA-receptor function
Indication- adjunctive therapy for partial sz

38
Q

Zonisamide (Zonegran) pharmacokinetics and Side effects

A

Good oral absorption and renally and hepatically eliminated
Side effects: Dose related: sedation, dizziness, cognitive impairment, nausea
Non-dose related- rash, oligohydrosis, kidney stones

39
Q

Pregabalin (lyrica) Indication and side effects

A

Indication- adjunctive tx for partial onset sz, peripheral neuropathy, postherpatic neuralgia, fibromyalgia syndome
Side effects- dizziness, somnolence, dry mouth, PERIPHERAL EDEMA, blurred vision, weight gain

40
Q

Benzodiazepines

A

Act as positive allosteric modulators by enhancing channel gating in presence of GABA
Not indicated if sz already stopped or for maintenance therapy.

41
Q

Benzodiazepines ADRs

A

Infusion rate related to arrhythmias and hypotension
Respiratory depression
Impairment of consciousness

42
Q

Lorazepam (Ativan)

A

DOC for patient w/ IV access
Onset of action 3-5 min
Can cause vein irritation (Dilution of dose)

43
Q

Lorazepam (ativan) vs diazepam (valium)

A

Lorazepam is preferred over diazepam secondary to duration of action
Diazepam highly lipophilic and quickly redistributes out of brain to other fat stores.
Diazepam DOA- 15 min to 2 hrs
Lorazepam DOA- 12-24 hrs

44
Q

Diazepam (valium)

A

Rapid onset, short duration

option if IV route not available (rectally)

45
Q

Midazolam (versed)

A

Reserved for refractory sz
Buccal, intranasal, IM routes
Give by continuos infusion for refractory SE

46
Q

Hydantoins place in therapy

A 
Second line (loading dose) if sz continue after 2-3 doses of benzos
Consider loading dose and maintenance dose if sz recur or if recurrence anticipated
Initiate maintenance doses 12-14 hrs after loading dose
Less CNS and respiratory depression than benzo and barbituates
47
Q

Hydantoins Side effects

A

Arrhythmias, nystagmus, dizziness, ataxia

48
Q

Phenytoin Onset of action and administration

A

Onset of Action- longer time to stop sz than benzos, less lipid soluable and requres slower administration
Admin- erractic absorption and pain w/ IM injections
Dilute with NS
Contains propylene glycol (result in arrhythmias, hypotension, metabolic acidosis with repeated doses)

49
Q

Fosphenytoin (Cerebyx)

A

H20 soluble prodrug of phenytoin converted by plasma esterases
Available IM and IV
Doesn’t contain propylene glycol
Compatible with most IV solutions w/ less phlebitis
Paresthesias and pruritis are more frequent

50
Q

Phenobarbital

A

3rd line agent, if sz persists despite 2-3 doses of benzos and loading dose of hydantoin
2nd line agent if sz persists after 2-3 doses of benzos and hydantoins contraindicated
Used in pediatric patients
Onset of action w/in minutes of loading dose administration

51
Q

Phenobarbital ADR

A

More CNS and respiratory depression than hydantoins

Contains propylene glycol

52
Q

NSAIDs

A

Non-specific meds for migraines
FIrst line for mild to moderate migraines.
Inhibit prostaglandin synthesis (inhibits inflammation in trigeminovascular system)
Includes- ASA (aspirin), naproxen, ibuprophen, APAP + ASA + Caffeine (Excedrin Migraine)

53
Q

What are the first line NSAIDs?

A

ASA (aspirin), naproxen, ibuprophen, APAP (acetaminophen) + ASA + Caffeine (Excedrin Migraine)

54
Q

Butorphanol (Stadol nasal spray)

A

Synthetic narcotic antagonist-agonist

Abuse potential

55
Q

Barbiturate Combinations (hypnotics)

A

Non-specific migraine treatment
Combined w/ analgesics or codein
Potential for overuse, mod-severe migraine
EX- butalbital, aspirin & caffeine (fiorinal)

56
Q

What are the drug interactions of barbiturate combinations (hypnotics)?

A

Effects reduced by barbiturates- phenotiazine, quinidine, cyclosporine, theophylline, & BETA BLOCKERS
Effects increased by barbiturates- chloramphenicol, benzodiazepines, CNS depressents

57
Q

Ergot Alkaloids-MOA

A

5-HT1 agonist, activity of alpha, beta-adrenergic receptors and DA receptors

  • Constricts intracranial blood vessels
  • Inhibits development of neurogenic inflammation in the trigeminovascular system
58
Q

Ergotamine tartrate pharmacokinetics

A

Oral tablet and retal tablet

59
Q

Dihydroergotamine

A

Nasal spray

60
Q

Ergotamine acute side effects

A 
N/V (pretreatment with antiemetic)
Diarrhea
Abdominal pain
Weakness
Leg cramps
Tremor
Dizziness
Syncope
Chest pain
Intermittent Claudication
Syndrome of ergotism
61
Q

Ergotamine chronic side effects

A 
Cerebral/peripheral ischemic disorders
Hypertension
TACHY/BRADY
Medication overuse HA
Renal D/O
Withdrawal signs: severe HA, N/V, malaise
62
Q

Ergotamine Contraindications

A 
Sepsis
Renal/hepatic failure
Pregnancy/lactation
Gluacoma
Peptic ulcer disease
Uncontrolled HTN
CHD/Stroke/PVD
Potential interactions w/ protease inhibitors
USE OF TRIPTANS W/IN 24 HOURS
63
Q

Ergotamine Drug Interactions

A

CYP 3A4 substrate
Interactions w/ strong 3A4 inhibitors (azole antifungals, macrolides, protease inhibitors)
Triptans (additive vasoconstrictive effect)
Fluoxetine, fluvoxamine (competes for metabolism by 3A4)

64
Q

Triptans

A

Selective 5-HT1b/d agonists- intracranial vasoconstriction, inhibition of neuropeptide release from trigeminovascular nerves, interrupts pain signal w/in brain stem trigeminal nuclei
1ST LINE FOR MODERATE TO SEVERE MIGRAINE

65
Q

Triptan- sumatriptan (imitrex)- ROA

A

SQ injection, oral tabs, nasal spray

66
Q

Triptans- Rizatriptan (Maxalt)-ROA

A

Oral tabs, oral disintegrating tabs

67
Q

Zolmitriptan (Zomig)

A

Oral tabs, oral disintegrating tabs, nasal spray

68
Q

Triptan Side effects

A 
Dizziness
Fatigue
Flushing
Nausea
Chest tightness, pressure, heaviness, pain
Injection rxn
Taste perversion from nasal spray
69
Q

Triptan Contraindications

A 
Ergot alkaloid in last 24 hrs
MAOI in last two weeks
Ischemic heart disease/cerebrovascular
Uncontrolled HTN
Hemiplegic and basilar migraines
70
Q

Triptan- drug interactions

A 
MAOI:  inhibits clearance of triptans
Risk of serotonin syndrome
SSRIs
Risk of serotonin syndrome
Ergotamine containing products
Increased vasoconstrictive effects
71
Q

Beta-blockers MOA and contraindications

A

1st line agents for prophylactic treatment- agents include propranalol (inderal), metoprolol (lopressor), atenolol(tenormin), & nadolol
MOA- unknown theory is that it may regulate serotonin transmission in cortical pathways
Contraindications- pts w/ peripheral vascular disease, depression, asthma

72
Q

Beta-blocker ADRs

A

Fatigue, vivid dreams, depression, impotence, BRADYCARDIA, HYPOTENSION

73
Q

Tricyclic antidepressants (TCAs) MOA

A

Also used as 1st line agents for migraines- include imipramine (tofranil), nortriptyline (pamelor), & AMITRIPTYLINE (elavil)
MOA- antagonist of 5-HT2 receptors inhibiting the reuptake of serontonin and causing increased concentration of serotonin in the synaptic cleft

74
Q

Tricyclic antidepressants (TCAs) ADRs and Drug interactions

A

ADRs-Sedation, constipation, blurred vision, HPOTN

Drug interactions- MAOIs

75
Q

Valproic acid (depakene) and divalproex sodium (depakote) MOA and contraindications

A

Anticonvulsant
MOA- increased activity of GABA inhibitory transmitter
Contraindications- liver-disease, monitor liver enzymes

76
Q

Valproic acid (depakene) and divalproex sodium (depakote) ADRs and drug interactions

A

Anticonvulsant
ADRs- tremor, weight gain, hair loss, nausea
Drug interactions- other anticonvulsants, CNS depressants, absence sz in combo w/ clonazepam

77
Q

What other anticonvulsants besides Valproic acid (depakene) and divalproex sodium (depakote) can be used in the prophylaxis of migraines?

A

Carbamazepine (tegretol), topiramate (topamax), gabapentin (neurontin)

78
Q

Calcium channel blockers

A

Verapamil, nimodipine, diltiazem

Vasodilators that cause decrease in smooth muscle tone and vascular resistance

79
Q

Methysergide (Sansert)

A

Should not be used unless nothing else worse and a patient has severe migraines due to black box warning of fatal pulmonary fibrosis
MOA- peripheral 5-HT inhibitor but central 5-HT agonist
Use only for 6 mo. followed by 3-4 week drug free period.
Effective but has serious side effects

80
Q

Botulinum Toxin Type A (Botox)

A

Prophylaxis of migraines
Inhibits acetylcholne release at the presynaptic cholinergic junction (inhibition of overactive peripheral neurons, possibly modulates substance P, and does not cross BBB)
Not FDA approved indication
Prophylactic effect seen 60-90 days after injection
Inconsistent clinical trials

Pharmacology II (23 decks)

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