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Systemic Pharm Final > Analgesics > Flashcards

Analgesics Flashcards

1
Q

Tramadol drug interactions?

A

Anticholinergics -additive constipation/paralytic ileus.
Classic Antihistamines -additive CNS depression.
Azoles (Antifungal) -impaired drug metabolism.
Antagonizes ACh receptors (both muscarinic and nicotinic).

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2
Q

Celecoxib drug interactions?

A

NSAIDs (esp Ketorolac), Corticosteroids -hemorrhage.

Azoles (anti fungals) -impaired metabolism.

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3
Q

Aspirin drug Interactions?

A

NSAIDs and Omega 3 -Additive risk of hemorrhage.

Acetaminophen and Cyclosporine -Additive nephrotoxicity (liver toxicity).

Steroids -Additive gastrointestinal toxicity.

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4
Q

Sumatriptan drug interactions?

A

No Ocular Drug Interactions.

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5
Q

Acetaminophen drug interactions?

A

Acetaminophen/antihistaminic Combos -Additive hepatotoxicity (liver toxicity).

ASA -Additive nephropathy (damage to kidneys).

Lidocaine Topical -Additive methemoglobinemia (too much methemoglobin, hemoglobin in the F3 state instead of the F2 state, in the blood. In the F3 state the hemoglobin cannot bind oxygen to carry it throughout the body).

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6
Q

Ergotamine drug interactions?

A

Macrolides, Fluoroquinolones, Cyclosporine, Azole (antifungal) -inhibit the drug’s metabolism.
Tetracyclines may increase risk of ergot toxicity.
Timolol enhances peripheral vasoconstriction.

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7
Q

Hydrocodone/Acetaminophen drug interactions?

A

Anticholinergics -additive constipation/paralytic ileus
Classic Antihistamines -additive CNS depression.
Carbonic Anhydrase Inhibitors (CAIs) -Impairs renal excretion of carbonic anhydrase inhibitors (CAIs), leading to CNS toxicity, metabolic acidosis.
Renal impairment would be greater with aspirin (ASA) versus Acetaminophen.

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8
Q

Topiramate drug interactions?

A

Carbonic Anhydrase Inhibitors (CAIs), Steroids -additive hypokalemia (low blood Potassium level).

Fluoroquinolones -QT prolongation.

Opioids, Classic Antihistamines -increased risk of CNS depression.

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9
Q

What is the mechanism of action for topiramate?

A 
Migraine, headache and seizure disorder prophylactic.
Blocks voltage-gated sodium channels.
Carbonic Anhydrase Inhibitor (CAI).
Antagonizes glutamate receptors.
Enhances GABA activity.
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10
Q

What is the mechanism of action for acetaminophen?

A

Non-NSAID analgesic.
Acts by inhibiting cyclooxygenase (COX), prostaglandin (PG) synthetase, and enhancing serotonin (5-HT) release (attenuates pain mediator generation).
Regulates body temperature by acting centrally at the hypothalamus.

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11
Q

What is the mechanism of action for celecoxib?

A

NSAID.

Selectively inhibits COX-2 (cyclooxygenase 2) and reduces prostaglandin (PG) synthesis.

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12
Q

What is the mechanism of action for hydrocodone?

A

Analgesic and Antitussive (stops cough) Synthetic Opioid.
Acts through G-Protein-Coupled Mu, Kappa & Delta ‘opioid’ receptors.
Inhibits adenylyl cyclase activity.
Enhances potassium (K+) outflow.
Hyperpolarizes nerves affecting neuronal excitability and muscle tone.
Stimulates prolactin and growth hormone release.

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13
Q

What is the mechanism of action for sumatriptan?

A

Migraine and headache abortive.
Selectively activates vascular serotonin (5HT-1) receptors, producing intracranial vasoconstriction
Stimulate neuronal serotonin receptors, decreasing the release of peptides including Substance P (Pain signal propagator) and Calcitonin Gene Related Peptide.

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14
Q

What is the mechanism of action for tramadol?

A

Central Acting Synthetic Opioid Analgesic.
Agonist at mu receptors and weak inhibitor of norepinephrin (NE) /serotonin (5-HT) reuptake. (weak SNRI)
Mu agonist effect is greater with active metabolite.

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15
Q

What is the mechanism of action for ASA?

A

NSAID.
Irreversibly, non-selectively inhibits cyclooxygenase (COX), reducing prostaglandins (PG) and thromboxin A2 (TXA2) synthesis.

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16
Q

What is the mechanism of action for ergotamine?

A

Migraine and headache abortive.
Structurally similar to biogenic amines.
Stimulates serotonin receptors producing
intracranial vasoconstriction; caffeine enhances vasoconstriction.
Inhibition of cranial nerve 5 ,the trigeminal nerve, pain transmission.

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17
Q

What is Hydrocodone used for?

A

Synthetic Opiate used for moderate to moderately severe pain.

18
Q

What are the progressive doses for therapeutic effects of ASA?

A

Anti Platelet 80-160mg (irreversible inhibition of COX1 for life of the platelet).
Analgisia 160-325mg peripheral > central.
Anti-pyretic 160-325mg.
Anti-Inflammatory 325-650mg (dangerous dose).

19
Q

What is aspirin used to treat?

A

Pain/Fever.
Arthritis.
MI/TIA.
(inflammation, peripheral > central pain relief, reduce clotting).

20
Q

What is celecoxib (Celebrex) used for?

A

Acute Pain.
Arthritis.
Ankylosing Spondylitis.
Dysmenorrhea (painful Menstruation).

21
Q

What is Topiramate used for?

A

This PROPHYLACTIC migraine therapy is used for Migraine Prophylaxis, Seizures.

22
Q

What is Tramadol used for?

A

Non-conventional Opioid used for moderate to moderately severe pain.

23
Q

What is acetaminophen used to treat?

A

Pain (centrally enhancing 5-HT serotonin generation).
Fever (no inflammation control).
Pain relief during pregnancy.

24
Q

What is Ergotamine used for?

A

It is used as ABORTIVE therapy for Migraines and Cluster Headaches. Derived from a fungus.

25
Q

What is Sumatriptan used for?

A

This ABORTIVE Migraine therapy used to abort Acute Migraines and Cluster Headaches.

26
Q

Contraindications of ASA?

A 
Hemorrhagic disorders.
Pregnancy (especially 3rd trimester).
Corneal denervation.
Dry eye.
NSAID/ASA induced asthma.
Active Peptic Ulcer.
Chronic gastrointestinal tract inflammation.
27
Q

Contraindications of Acetaminophen?

A

Liver Failure.
Liver Problems.
Kidney Problems.
Shock.

28
Q

Contraindications of Celecoxib?

A

Sulfonamide allergy.

29
Q

Contraindications of Hydrocodone/acetaminophen?

A

Mydriatic procedures (antagonized).

30
Q

Contraindications of Sumatriptan?

A

Caution in Hypertension.

31
Q

Contraindications of Topiramate?

A

Caution -Hemorrhage.

32
Q

NSAIDs block which pathway?

A

The Cyclooxygenase (COX) -> Arachidonate pathway Central Pathway.

33
Q

What is the pathway of Aspirin (mechanism)?

A

Prodrug of salicylic acid which irreversibly inhibits COX unlike actual NSAIDs. Also, reduces prostoglandin and thromboxin A2. Reduced clotting lasts the life of the platelet (7-10 days) because of the decreased thromboxin A2 (TXA2).

34
Q

What are the side effects of ASA

A

ADVERSE EFFECTS.
Common: bleeding time doubles, headache.
NOTABLE ADVERSE EFFECTS.
Hypersensitivity (non-immune): angioedema.

35
Q

What is Reye’s syndrome?

A

Adverse reaction in children to aspirin use for fever reduction associated with viral infections.
35% mortality rate.

36
Q

What are the side effects of acetaminophen?

A

ADVERSE EFFECTS.
Common: nausea, rash, headache.
SERIOUS ADVERSE EFFECTS.
Hepatic: acute hepatotoxicity usually w/ doses >4g/d.
Renal: acute renal tubular necrosis, chronic analgesic nephropathy.

37
Q

What are the side effects of celecoxib?

A 
ADVERSE EFFECTS.
Common: headache.
BLACK BOX WARNINGS.
CV: Stroke, Congestive Heart Failure (CHF) , myocardio Infarction (MI).
GI: Bleed, ulceration/perforation.
38
Q

What are the side effects of hydrocodone?

A

ADVERSE EFFECTS.
Common: lightheadedness, dizziness, sedation, miosis [no tolerance], pruritus (itching) & flushing (histamine release [little tolerance]).
CV: bradycardia/tachycardia; orthostatic hypotension.
CNS: drowsiness (tolerance in about 1 wk), mood changes (quick tolerance); elevated intracranial pressure (enhanced with head injury).

39
Q

What are the side effects of tramadol?

A 
ADVERSE EFFECTS.
Common: headache, pruritus, flushing.
CNS: Serotonin syndrome.
CVS: Orthostatic hypotension.
MIOSIS IS NOT A SIDE EFFECT because of mu selectivity.
40
Q

What are the side effects of sumatriptan?

A 
COMMON ADVERSE EFFECTS.
CNS: dizziness.
SERIOUS ADVERSE EFFECTS.
Hypersensitivity: angioedema.
Ocular: partial vision loss, transient/permanent blindness.
41
Q

What are the side effects of ergotamine?

A

ADVERSE EFFECTS.

Photosensitivity.

42
Q

What are the side effects of topiramate?

A

COMMON ADVERSE EFFECTS.
Bleeding.
Ocular: Nystagmus, diplopia, visual disturbance.
SERIOUS ADVERSE EFFECTS.
Ocular: Angle closure glaucoma, myopia, maculopathy.
Hemorrhage, anemia.

Systemic Pharm Final (12 decks)

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