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Pharmacology I > EXAM ONE DRUGS > Flashcards

EXAM ONE DRUGS Flashcards

PNS CNS

1
Q

PHENYTOIN

THERAPEUTIC USES

A

All forms of epilepsy EXCEPT absence seizures

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2
Q

PHENYTOIN

MECHANISM OF ACTION

A

TRADITIONAL ANTISEIZURE

Slows recovery of sodium channels from inactive to active state

Results in a blockade of sodium entry ONLY into hyperactive neurons

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3
Q

PHENYTOIN

SIDE EFFECTS

A

Toxicity: Nystagmus, sedation, ataxia, diplopia, cognitive impairment

Gingival Hyperplasia

Measles-ish rash that can progress to SJS or TEN

DRESS

Teratogen in pregnancy

IV: can cause cardiac dysrhythmias and hypoTN if given too quickly

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4
Q

PHENYTOIN

PATIENT EDUCATION

A
  1. Optimal Dose will take time to find
  2. Emphasize importance of strict adherence
  3. Danger of quick withdrawal
  4. Maintain a frequency chart
  5. Purpose and importance of lab draws
  6. No driving etc. until seizures controlled
  7. CNS depression may occur, don’t use with alcohol or other depressants
  8. Folic acid during pregnancy
  9. Watch for suicidal behavior
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5
Q

CARBAMAZEPINE

MECHANISM OF ACTION

A

TRADITIONAL ANTIPSYCHOTIC

Same as phenytoin: delays sodium channel recovery

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6
Q

CARBAMAZEPINE

THERAPEUTIC EFFECTS

A
  1. Tonic-clonic, simple partial, and complex partial
  2. Symptomatic control in bipolar refractory to lithium
  3. neuralgia associated with trigeminal and glossopharyngeal nn
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7
Q

CARBAMAZEPINE

ADVERSE EFFECTS

A

FEWER THAN PHENYTOIN

Minimal effects on cognitive function

Can have neurologic effects during the firs weeks of treatment, but usually reduced as use goes on

Bone marrow suppression

Aplastic Anemia (very rare), but all patients should have serial CBCs

Teratogenic

Promotes ADH secretion

Morbilliform rash, SJS, TEN, DRESS

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8
Q

CARBAMAZEPINE

PATIENT EDUCATION

A

Same as phenytoin. ALSO:

May inactivate oral contraceptives

Accelerates hepatic drug metabolism (may effect other drugs)

No grapefruit juice

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9
Q

LAMOTRIGINE

MECHANISM OF ACTION

A

Blocks sodium channels and partly blocks calcium channels as well

Both actions target decreases the release of glutamate

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10
Q

LAMOTRIGINE

THERAPEUTIC USES

A
  1. adjunctive therapy of partial seizures age > 2
  2. adjunctive therapy of generalized seizures with lennox-gastaut age > 2
  3. adjunctive therapy of primary generalized tonic-clonic seizures age > 2
  4. monotherapy for partial seizures age . 16
  5. long term maintenance of bipolar
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11
Q

LAMOTRIGINE

ADVERSE EFFECTS

A

Dizziness, diplopia, blurred vision, headache

N/V

SJS, TEN, DRESS

Blood dyscrasias

aspetic meningitis

Risk for suicide

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12
Q

BACLOFEN

MECHANISM OF ACTION

A

CENTRALLY ACTING

acts within the spinal cord to suppress hyperactive reflexes involved in muscle movement regulation

Structural analog of GABA, so maybe its mimicking the actions of GABA? No one is sure

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13
Q

BACLOFEN

THERAPEUTIC USES

A

Reduces spasticity from MS and spinal cord injury

decreases flexor and extensor spasms, suppresses resistance to passive movement

NO DIRECT MUSCLE RELAXATION

Not approved for management of spasticity r/t stroke, PD or Huntington

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14
Q

BACLOFEN

ADVERSE EFFECTS

A

CNS depression (usually only during early phase of therapy))

Withdrawal can cause hallucinations and seizures

N/V/ constipation, urinary retention

Hypotension

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15
Q

BACLOFEN

PATIENT EDUCATION

A

Possible depressant effects, avoid alcohol

Hypotension, nausea, vomiting, constipation

No abrupt discontinuation, taper over 1-2 weeks

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16
Q

CYCLOBENZAPRINE

MECHANISM OF ACTION

A

CENTRALLY ACTING

Used to treated localized muscle spasms

Reduces tonic motor activity in the brainstem

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17
Q

CYCLOBENZAPRINE

THERAPEUTIC USES

A

Acute muscle spasm and associated pain

The most efficacious drug for this purpose

NOT effective against spasticity

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18
Q

CYCLOBENZAPRINE

ADVERSE EFFECTS

A

CNS: drowsiness, dizziness, most intense early on and then lessen

Anticholinergic effects: structurally similar to Tricyclic antidepressants, so has some anticholinergic effects (xerostomia, photophobia, constipation etc)

Cardia rhythm disturbances (similar to tricyclics - ST, conduction delays)

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19
Q

CYCLOBENZAPRINE

PATIENT EDUCATION

A

Same as for others: CNS effects, avoid alcohol, etc

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20
Q

DANTROLENE

MECHANISM OF ACTION

A

DIRECT ACTING!

Acts within the skeletal muscles

Suppresses release of calcium from the SR

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21
Q

DANTROLENE

THERAPEUTIC USES

A

Relieves spasticity associated with MS, Cerebral Palsy, SCI

MALIGNANT HYPERTHERMIA

Causes a significant reduction in strength

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22
Q

DANTROLENE

ADVERSE EFFECTS

A

Hepatic Toxicity (need serial LFTs) - BAD black box warning

Muscle weakness

drowsiness

diarrhea

If given IV, ⅓ will have facial flushing

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23
Q

DANTROLENE

PATIENT EDUCATION

A

Possible depressant effects

liver dysfunction s/s

Avoid CNS depressants

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24
Q

LEVADOPA-CARBIDOPA

MECHANISM OF ACTION

A

Levadopa: undergoes conversion to dopamine in the brain and activates dopamine receptors

Carbidopa: inhibits decarboxylases - blocks destruction of levodopa in the periphery, allowing more to reach the brain

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25
Q

LEVADOPA-CARBIDOPA

THERAPEUTIC USES

A

First line drug for Parkinson Disease dyskinesias

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26
Q

LEVADOPA-CARBIDOPA

ADVERSE EFFECTS

A

N/V

Dyskinesias

Postural hypotension early in tx

Dyskinesias

Psychosis

CNS effects

Dark sweat and urine

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27
Q

LEVADOPA-CARBIDOPA

PATIENT EDUCATION

A

benefits may be delayed from weeks to months

possibility of “off” times and avoiding high protein meals

Take meds with low-fat, low-protein food to reduce nausea

levadopa-induced movement disorders

avoid child-proof containers for meds

cardiac sensitivity

increase salt intake or alpha agonist for hypoTN

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28
Q

AMANTADINE

MECHANISM OF ACTION

A

Antiviral agent that was found to be effective in PD

Lots of theories about how it does this

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29
Q

AMANTADINE

THERAPEUTIC USE

A

Relieving dyskinesias from levodopa

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30
Q

AMANTADINE

ADVERSE EFFECTS

A

confusion, light headedness, anxiety

effects from muscarinic blockade: blurred vision, urinary retention, dry mouth, constipation

May develop mottled discoloration of the skin (livedo reticularis)

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31
Q

AMANTADINE

PATIENT EDUCATION

A

Watch out for side effects

awareness that efficacy will decrease over time

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32
Q

ENTACAPONE

MECHANISM OF ACTION

A

COMT inhibitor

inhibits metabolism of levodopa in the periphery

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33
Q

ENTACAPONE

THERAPEUTIC USES

A

increases the efficacy of levadopa

Often combined with Levodopa and Carbamazepine in one formulation

Only downside is that taking all three as one dose limits the ability to titrate one or the other, so often given as a separate pill/dose

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34
Q

ENTACAPONE

ADVERSE EFFECTS

A

Can worsen the side effects of levodopa, because it’s increasing the amount that gets to the brain

Increases the levels of drugs metabolized by COMT like methyldopa, dobutamine, and isoproterenol

If they’re on these meds, will need REDUCED doses of those drugs, because they won’t metabolize them as quickly

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35
Q

ENTACAPONE

PATIENT EDUCATION

A

Vigilance for side effects

may need decreased dose of levodopa once entacapone is started

36
Q

PRAMIPEXOLE

MECHANISM OF ACTION

A

Non-ergot dopamine receptor agonist (unlike levodopa, it doesn’t become dopamine, it just activates the receptor like dopamine would)

direct activation of dopamine receptors in the striatum

37
Q

PRAMIPEXOLE

THERAPEUTIC USES

A

Used in early onset as monotherapy for PD

Used in late stage PD as an agonist with levodopa

It’s less effective at relieving motor dyskinesias, but it’s also less likely that levodopa to cause them

38
Q

PRAMIPEXOLE

ADVERSE EFFECTS

A

Monotherapy: nausea, dizziness, somnolence, insomnia, constipation, weakness, hallucinations

Associated with IMPULSE CONTROL DISORDERS

39
Q

PRAMIPEXOLE

PATIENT EDUCATION

A

Can cause sleep attacks

Screen for impulse disorders

Orthostatic hypotension

40
Q

TIZANIDINE

MECHANISM OF ACTION

A

Centrally acting muscle relaxant

exact MOA is unclear

maybe enhances presynaptic inhibition of motor neurons in the CNS

Acts as an agonist at presynaptic alpha 2 receptors

41
Q

TIZANIDINE

THERAPEUTIC USES

A

spasticity

off label: acute back pain

42
Q

TIZANIDINE

ADVERSE EFFECTS

A

CNS depression

hepatic toxicity

Physical dependence

hypotension (very similar to clonidine)

dry mouth, hypotension, hallucinations, psych s/s

43
Q

TIZANIDINE

PATIENT EDUCATION

A

Possibility for CNS depression

risk of falls

avoid alcohol and first-generation antihistamines to avoid double CNS depression

Don’t discontinue abruptly

withdrawal will ensure

44
Q

PYRIDOSTIGMINE

MECHANISM OF ACTION

A

Reversible cholinesterase inhibitor

acts as a substrate for cholinesterase, tying it all up so that Ach can remain in circulation

45
Q

PYRIDOSTIGMINE

THERAPEUTIC USES

A

Myasthenia Gravis

46
Q

PYRIDOSTIGMINE

ADVERSE EFFECTS

A

Excessive muscarinic stimulation: salivation, gastric secretion, increased tone/motility in GI tract, bradycardia, sweating, miosis

neuromuscular blockade: causes accumulation of Ach at the NMJ, preventing repolarization of mm cells

47
Q

PYRIDOSTIGMINE

PATIENT EDUCATION

A
  • Take before engaging in rigorous activity
  • If you miss a dose, don’t take another one until the scheduled time
  • report SOB, drooling, N/V/D, excessive sweating
  • Keep a list of medications on your person in case you have an attack
48
Q

DONEPEZIL

MECHANISM OF ACTION

A

Cholinesterase Inhibitor

Prevents the breakdown of Ach, enhancing transmission by central cholinergic neurons

More selective for the form of AChE in the brain that that found in the periphery

49
Q

DONEPEZIL

THERAPEUTIC USES

A

Mild to Severe Alzheimer’s Disease

50
Q

DONEPEZIL

ADVERSE EFFECTS

A

N/V/D

Bradycardia, Fainting Spells, Falls, Fall-related injuries

51
Q

DONEPEZIL

PATIENT EDUCATION

A
  • Explain that the drug likely will not dramatically improve symptoms (Only 1 in 12 see improvement)
  • Lightheadedness and risk for falls
  • Frequent snacks and meals to maintain weight
  • keep a list of new symptoms and problems for follow up appointments
52
Q

OXYBUTYNIN

MECHANISM OF ACTION

A

Muscarinic Antagonist

Competitively blocks the actions of Ach at muscarinic receptors, primarily at M3

53
Q

OXYBUTYNIN

THERAEUTIC USES

A

Overactive Bladder (OAB) (urge incontinence, not stress incontinence)

54
Q

OXYBUTYNIN

ADVERSE EFFECTS

A
  • Dry mouth, constipation, tachycardia, urinary retention
  • mydriasis, blurred vision
  • confusion, hallucinations, insomnia, agitation
  • metabolized by CYP3A4
55
Q

OXYBUTYNIN

PATIENT EDUCATION

A
  • sipping fluids/gum/saliva substitute for xerostomia
  • sunglasses and dim lighting
  • void right before taking to avoid retention
  • increase dietary fiber, use mild laxatives
  • avoid heat, at risk for hyperthermia
56
Q

ATROPINE

MECHANISM OF ACTION

A

Muscarinic Antagonist

Competitive blockade of muscarinic receptors, preventing ACh action

57
Q

ATROPINE

THERAPEUTIC USES

A
  • Preanesthetic to prevent reflex bradycardia and copious secretions
  • dilating eyes for examinations and surgery
  • Bradycardia
  • Intestinal hypertonicity and hypermotility
  • PUD
  • Asthma
  • Biliary Colic
  • Muscarinic agonist poisoning
58
Q

ATROPINE

ADVERSE EFFECTS

A
  • Xerostomia
  • Blurred Vision/Photophobia
  • Elevated IOP
  • urinary retention
  • constipation
  • anhidrosis (can’t sweat)
  • Tachycardia
  • Asthma (thickens secretions)
59
Q

ATROPINE

PATIENT EDUCATION

A

Same as for other muscarinic antagonists:

  • risk for hyperthermia
  • don’t drive with blurry vision
  • sugar free gum for xerostomia
  • pee before taking
60
Q

SCOPOLAMINE

MECHANISM OF ACTION

A

Anticholinergic drug similar to atropine

BUT

produces sedation instead of excitation

suppresses emesis and motion sickness

61
Q

SCOPOLAMINE

THERAPEUTIC EFFECTS

A
  • motion sickness
  • preanesthetic sedation
  • obstetric amnesia
62
Q

SCOPOLAMINE

ADVERSE EFFECTS

A

Same as atropine

63
Q

SCOPOLAMINE

PATIENT EDUCATION

A

Same as atropine, but explain risk for oversedation

no major life decisions etc.

no other CNS depressants

64
Q

IPRATROPRIUM

MECHANISM OF ACTION

A

Muscarinic Antagonist

Causes bronchodilation

65
Q

IPRATROPRIUM

THERAPEUTIC USES

A

Asthma, Rhinitis, COPD

66
Q

IPRATROPRIUM

ADVERSE EFFECTS

A
  • bronchitis
  • nausea
  • xerostomia, reduced secretions
  • paradoxical bronchospasms
67
Q

IPRATROPRIUM

PATIENT EDUCATION

A
  • best for chronic control, not acute
  • urinary retention possible
  • dry mouth etc.
68
Q

NOREPINEPHRINE

RECEPTOR SPECIFICITY

CHEMICAL CLASSIFICATION

A
  • Alpha 1
  • Alpha 2
  • Beta 1

Catecholamine

69
Q

NOREPINEPHRINE

PHYSICAL EFFECTS

A
  • Elicits all the responses as epinephrine, except that it does not activate Beta 2
  • Used to tried hypotension and cardiac arrest
70
Q

DOPAMINE

RECEPTOR SPECIFICITY

CHEMICAL CLASSIFICATION

A

CATECHOLAMINE

  • Dopamine
  • Beta 1
  • Alpha 1
71
Q

DOPAMINE

PHYSICAL EFFECTS

A
  • Dose Dependent
    • Low: Dopamine (renal vasodilation)
    • Medium: Beta 1 (cardiac output)
    • High: Alpha 1 (vasoconstriction)
72
Q

ALFUZOSIN / PRAZOSIN / TAMSULOSIN

CLASSIFICATION

A

SELECTIVE ALPHA 1 BLOCKERS

73
Q

ALFUZOSIN / PRAZOSIN / TAMSULOSIN

THERAPEUTIC USES

A

Alfuzosin: BPH only

Prazosin: HTN, off label BPH

Tamsulosin: BPH only

74
Q

ALFUZOSIN / PRAZOSIN / TAMSULOSIN

ADVERSE EFFECTS

A
  • Alfuzosin: Dizziness
  • Prazosin: Orthostatic HypoTN, reflex tachycardia, nasal congestion, “first dose effect”
  • Tamsulosin: Abnormal ejaculation, rhinitis
75
Q

ALFUZOSIN / PRAZOSIN / TAMSULOSIN

PATIENT EDUCATION

A
  • First-dose hypotension (prazosin mostly)
  • Avoid driving for 24 hours after first dose
  • Take initial dose at bedtime
  • home monitoring of BP and HR required, and patient should not take/call doctor if they develop bradycardia or hypoTN
76
Q

PROPANOLOL

MECHANISM OF ACTION

A

First generation non-selective Beta Blocker

Blocks cardiac beta 1 receptors

77
Q

PROPANOLOL

THERAPEUTIC USES

A
  • Beta 2
    • Bronchoconstriction
    • Vasoconstriction
    • Reduced glycogenolysis
  • Beta 1
    • Reduced Heart Rate
    • Negative inotrope
    • Suppresses impulse conduction through the AV node
    • Suppresses secretion of renin
78
Q

CLONIDINE

MECHANISM OF ACTION

A

Centrally acting Alpha 2 Agonist

Reduces presynaptic synthesis of NE

79
Q

CLONIDINE

THERAPEUTIC USES

A
  • Hypertension
  • Severe pain
  • ADHD
80
Q

CLONIDINE

ADVERSE EFFECTS

A
  • Drowsiness
  • Xerostomia
  • Rebound hypertension
  • Abuse
81
Q

CLONIDINE

PHARMACOLOGIC EFFECTS

A
  • Bradycardia
  • Decreased CO
  • Vasodilation
  • Decreased BP
82
Q

CLONIDINE

PATIENT EDUCATION

A
  • Take major portion at bedtime to minimize sedation
  • Patches aren’t MRI safe
  • Record BP daily
  • Don’t discontinue abruptly
  • CNS depression
  • Dry mouth measures
83
Q

DICYCLOMINE

MECHANISM OF ACTION

A

Muscarinic Antagonist

84
Q

DICYCLOMINE

THERAPEUTIC USES

A

a.k.a. Bentyl

IBS

Diarrhea and Hypermotility

85
Q

DICYCLOMINE

ADVERSE EFFECTS

A
  • Dry mouth
  • Blurred vision
  • Urinary retention
  • Constipation
  • Risk for hyperthermia

Pharmacology I (29 decks)

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