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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
Gabapentin (Neurotin) favorable pharmacokinetic profile
Dose-dependent oral absorption Not protein bound Excreted unchanged via kidneys No serum level monitoring
26
Gabapentin (Neurotin) Side effects
Somnolence, dizziness, ataxia, nystagmus
27
Tiagabine (Gabitril) MOA and Indication
Competitive inhibitor of GABA transporter in neurons and glia (inhibitors re-uptake) Indication- adjunctive tx of partial sz TAKE WITH FOOD
28
Tiagabine (Gabitril) pharmacokinetics and side effects
Quickly and completely absorbed Increased clearance in peds, with enzyme inducers Serum concentrations unnecessary Side effects- Dose related: dizziness, fatigue, nervousness, difficulty concentrating
29
Lamotrigine (lamictal) MOA and indication
Blocks Na+ and Ca++ channels Adjunctive in children and mono therapy in adults Indications- GTC, partial seizures, absence
30
Lamotrigine (lamictal) adverse side effects
Rash (10%), confusion, depression, N/V, diplopia, severe idiosyncratic (skin, blood) Slow taper essential, initial dose dependent on other meds
31
Topiramate (Topamax) MOA and indication
Blocks Na+ channels and binds GABA thus opening Cl- channels | Indication- tx for partial and generalized sz in pediatrics and adults.
32
Topiramate (Topamax) pharmacokinetics and adverse effects
``` 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 ```
33
Felbamate (felbtol) MOA and indication
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
Felbamate (felbtol) Side effects
Dose related- anorexia, N/V, insomnia, HA | Non-dose related- aplastic anemia, hepatic failure
35
Levetiracetam (Keppra) MOA and indication
MOA unknown Indication- tx of generalized sz Adjust dose in renal insufficiency
36
Levetiracetam (Keppra) favorable PK profile and Side effects
Almost completely absorbed Metabolism NOT dependent on the P450 system Minimal protein binding MInimal drug interactions Side effects- sedation, behavioral abnormalities
37
Zonisamide (Zonegran) MOA and Indication
Sulfonamide derivative: blocks Na+ and Ca++ channels and enhances GABA-receptor function Indication- adjunctive therapy for partial sz
38
Zonisamide (Zonegran) pharmacokinetics and Side effects
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
Pregabalin (lyrica) Indication and side effects
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
Benzodiazepines
Act as positive allosteric modulators by enhancing channel gating in presence of GABA Not indicated if sz already stopped or for maintenance therapy.
41
Benzodiazepines ADRs
Infusion rate related to arrhythmias and hypotension Respiratory depression Impairment of consciousness
42
Lorazepam (Ativan)
DOC for patient w/ IV access Onset of action 3-5 min Can cause vein irritation (Dilution of dose)
43
Lorazepam (ativan) vs diazepam (valium)
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
Diazepam (valium)
Rapid onset, short duration | option if IV route not available (rectally)
45
Midazolam (versed)
Reserved for refractory sz Buccal, intranasal, IM routes Give by continuos infusion for refractory SE
46
Hydantoins place in therapy
``` 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
Hydantoins Side effects
Arrhythmias, nystagmus, dizziness, ataxia
48
Phenytoin Onset of action and administration
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
Fosphenytoin (Cerebyx)
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
Phenobarbital
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
Phenobarbital ADR
More CNS and respiratory depression than hydantoins | Contains propylene glycol
52
NSAIDs
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
What are the first line NSAIDs?
ASA (aspirin), naproxen, ibuprophen, APAP (acetaminophen) + ASA + Caffeine (Excedrin Migraine)
54
Butorphanol (Stadol nasal spray)
Synthetic narcotic antagonist-agonist | Abuse potential
55
Barbiturate Combinations (hypnotics)
Non-specific migraine treatment Combined w/ analgesics or codein Potential for overuse, mod-severe migraine EX- butalbital, aspirin & caffeine (fiorinal)
56
What are the drug interactions of barbiturate combinations (hypnotics)?
Effects reduced by barbiturates- phenotiazine, quinidine, cyclosporine, theophylline, & BETA BLOCKERS Effects increased by barbiturates- chloramphenicol, benzodiazepines, CNS depressents
57
Ergot Alkaloids-MOA
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
Ergotamine tartrate pharmacokinetics
Oral tablet and retal tablet
59
Dihydroergotamine
Nasal spray
60
Ergotamine acute side effects
``` N/V (pretreatment with antiemetic) Diarrhea Abdominal pain Weakness Leg cramps Tremor Dizziness Syncope Chest pain Intermittent Claudication Syndrome of ergotism ```
61
Ergotamine chronic side effects
``` Cerebral/peripheral ischemic disorders Hypertension TACHY/BRADY Medication overuse HA Renal D/O Withdrawal signs: severe HA, N/V, malaise ```
62
Ergotamine Contraindications
``` 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
Ergotamine Drug Interactions
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
Triptans
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
Triptan- sumatriptan (imitrex)- ROA
SQ injection, oral tabs, nasal spray
66
Triptans- Rizatriptan (Maxalt)-ROA
Oral tabs, oral disintegrating tabs
67
Zolmitriptan (Zomig)
Oral tabs, oral disintegrating tabs, nasal spray
68
Triptan Side effects
``` Dizziness Fatigue Flushing Nausea Chest tightness, pressure, heaviness, pain Injection rxn Taste perversion from nasal spray ```
69
Triptan Contraindications
``` Ergot alkaloid in last 24 hrs MAOI in last two weeks Ischemic heart disease/cerebrovascular Uncontrolled HTN Hemiplegic and basilar migraines ```
70
Triptan- drug interactions
``` MAOI: inhibits clearance of triptans Risk of serotonin syndrome SSRIs Risk of serotonin syndrome Ergotamine containing products Increased vasoconstrictive effects ```
71
Beta-blockers MOA and contraindications
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
Beta-blocker ADRs
Fatigue, vivid dreams, depression, impotence, BRADYCARDIA, HYPOTENSION
73
Tricyclic antidepressants (TCAs) MOA
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
Tricyclic antidepressants (TCAs) ADRs and Drug interactions
ADRs-Sedation, constipation, blurred vision, HPOTN | Drug interactions- MAOIs
75
Valproic acid (depakene) and divalproex sodium (depakote) MOA and contraindications
Anticonvulsant MOA- increased activity of GABA inhibitory transmitter Contraindications- liver-disease, monitor liver enzymes
76
Valproic acid (depakene) and divalproex sodium (depakote) ADRs and drug interactions
Anticonvulsant ADRs- tremor, weight gain, hair loss, nausea Drug interactions- other anticonvulsants, CNS depressants, absence sz in combo w/ clonazepam
77
What other anticonvulsants besides Valproic acid (depakene) and divalproex sodium (depakote) can be used in the prophylaxis of migraines?
Carbamazepine (tegretol), topiramate (topamax), gabapentin (neurontin)
78
Calcium channel blockers
Verapamil, nimodipine, diltiazem | Vasodilators that cause decrease in smooth muscle tone and vascular resistance
79
Methysergide (Sansert)
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
Botulinum Toxin Type A (Botox)
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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