Pharm II - Test 1 Flashcards
Class: Morphine (MS Contin)
Opioid analgesic
MOA: Morphine (MS Contin)
Opioid receptor agonist
Indication: Morphine (MS Contin)
Pain relief
Acute MI
Properties: Morphine (MS Contin)
Analgesic
Anxiolytic
Vasodilator
Side effects: Morphine (MS Contin)
Respiratory depression Miosis Itching (dt histamine release) N/V Constipation (paralytic ileus)
Class: Fentanyl/Duragesic
Opioid analgesic
Indication: Fentanyl/Duragesic
Pain relief, anesthesia
MOA: Fentanyl/Duragesic
Opioid receptor agonist
80x the analgesic property of morphine
Route: Fentanyl/Duragesic
IV, transdermal patch, buccal lozenge/film, SL spray, lollypop
Contraindications: Fentanyl/Duragesic
Direct use with heating pads (inc. dose)
Class: Codeine
Opioid analgesic
MOA: Codeine
Opioid agonist, converted to morphine, much weaker analgesic than morphine
Contraindications: Codeine
CYP2D6 polymorphism, which causes ultra-rapid metabolism of codeine
Side effects: Codeine
Sedation
Constipation
Itching
Indication: Tramadol/Ultram
Withdrawal of heroin and morphine
Class: Naloxone (Narcan)
Opioid antagonist
Indication: Naloxone (Narcan)
Opioid overdose
Reverses coma/respiratory depression
MOA: Naloxone (Narcan)
Opioid antagonist (bind w/ high affinity, but do not activate response)
Class: Aspirin / Acetylsalicyclic acid (ASA)
NSAID (COX 1/2 inhibitor)
MOA: Aspirin / Acetylsalicyclic acid (ASA)
Irreversible inhibition of COX-1 and COX-2 enzymes -> blockade of prostaglandin synthesis
Why is aspirin not indicated for post-surgery?
Irreversibly affects platelets
Side effects: Aspirin / Acetylsalicyclic acid (ASA)
Inc. risk of Reye’s syndrome
Salicylism
dizziness, tinnitus, hyperventilation, mental status changes, potential for coma/death
Tx: Salicylism
IV hydration, alkalinization of urine, dialysis if necessary
Class: Ibuprofen (Motrin, Advil)
NSAID (COX 1/2 inhibitor)
MOA: Ibuprofen (Motrin, Advil)
Reversible inhibition of COX-1 and COX-2 enzymes
Class: Celecoxib (Celebrex)
NSAID (selective COX-2 inhibitor)
Indication: Celecoxib (Celebrex)
adenomatous polyps
MOA: Celecoxib (Celebrex)
Reversible, selective COX-2 inhibition
Class: Acetaminophen (Tylenol)
NSAID
Acetaminophen (Tylenol) is pregnancy category __.
B
Stage 1 - Acetominophen toxicity
12-24 hrs - N/V
Stage 2 - Acetominophen toxicity
24-48 hrs - mb clinically improved, but rising AST, ALT, bilirubin levels
Stage 3 - Acetominophen toxicity
72-96 hrs - peak hepatotoxicity, AST mb > 20,000
Stage 4 - Acetominophen toxicity
> 96 hrs - recovery, LV transplant or death
Antidote - Acetominophen toxicity
N-acetylcysteine within 8 hours of OD
What serotonin receptor elicits vasoconstriction?
Serotonin 1 (5 HT-1)
What serotonin receptor elicits vasodilation?
Serotonin 2 (5 HT-2)
Indication: Propranolol (Inderal)
HTN, angina, AMI, panic attacks, migraines (prophylaxis), hyperthyroidism
Contraindications: Amitriptyline (Elavil)
Do not use with monoamine oxidase (MAO) inhibitors
Class: Topiramate (Topamax)
Anticonvulsant
Inidication: Topiramate (Topamax)
Epilepsy, migraines (prophylaxis), weight loss, bipolar d/o (off-label)
MOA: Topiramate (Topamax)
Block voltage-dependent Na channels in CNS -> affects GABA activity
Class: Methysergide (Sansert)
Ergot derivative (serotonin 2 antagonist)
Indication: Methysergide (Sansert)
Migraine (prophylaxis) and cluster HA
MOA: Methysergide (Sansert)
Serotonin 2 receptor antagonist
Contraindications: Methysergide (Sansert)
Should not be used longer than 6 months
Do not use within 24 hrs of a triptan bc of inc. risk of vasoconstrictive spasm
Category X
Prodromal phase of migraines medications (1)
Sumatriptan (Imitrex)
Prophylaxis of migraines medications (4)
Propranolol (Inderal)
Amitryptyline (Elavil)
Methysergide (Sansert)
Topiramate (Topamax)
Indication: Sumatriptan (Imitrex)
Migraine and cluster HA
MOA: Sumatriptan (Imitrex)
Serotonin agonist at 5-HR 1D/1B receptors
Side effects: Sumatriptan (Imitrex)
Serotonin syndrome
Contraindications: Sumatriptan (Imitrex)
Use w/ caution in pts with HTN or angina
Category C
Serotonin syndrome
agitation, tremor, ataxia, fever, chills, diarrhea
Class: Butorphanol (Stadol)
Opioid analgesic
Indication: Butorphanol (Stadol)
Migraine HA refractory to triptans
MOA: Butorphanol (Stadol)
Mixed agonist-antagonist of opioid receptors
Anti-emetic for migraines medications (1)
Prochlorperazine (Compazine)
Category: Ondansetron (Zofran)
Antiemetic
MOA: Ondansetron (Zofran)
Blockade of serotonin (5HT3) receptor sites
If a patient is taking Aspirin and you add an NSAID, ___
you reduce the cardioprotective effects of aspirin
Treatment of acute gouty attack includes:
NSAIDs
Steroids
Colchicine
Prophylactic tx of gout includes:
Colchicine
Allopurinol
Probenecid
Category: Indomethacin (Indocin)
NSAID
Indication: Indomethacin (Indocin)
Gout, arthritis, bursitis, migraine, hemicrania, pain, swelling
MOA: Indomethacin (Indocin)
COX-I and COX-II inhibition
Category: Colchicine
Mitotic inhibitor
Indication: Colchicine
Gout (acute and prophylaxis)
MOA: Colchicine
Inhibits microtubule polymerization via tubulin binding -> Tubulin essential for mitosis
Inhibits neutrophil motility/activity -> anti-inflammatory
Side effects: Colchicine
PERIPHERAL NEUROPATHY, GI upset, anemia, neutropenia, hair loss
Category: Allopurinol (Zyloprim)
Purine analog
Indication: Allopurinol (Zyloprim)
Hyperuricemia, gout, prophylaxis against tumor lysis syndrome
MOA: Allopurinol (Zyloprim)
Xanthine oxidase inhibitor
Category: Probenecid (Probalan)
Uricosuric
Indication: Probenecid (Probalan)
Hyperuricemia, gout
MOA: Probenecid (Probalan)
Interferes w/ kidneys’ organic anion transporter (OAT), which normally retains uric acid from urine
Contraindications: Probenecid (Probalan)
Pts with G6PD deficiency (hemolytic anemia)
Pts w/ renal insufficiency (formation of uric acid stones)
Use w/ salicylates
PARQ: Probenecid (Probalan)
Drink water, stay hydrated to prevent stone formation
Side effects: corticosteroids
Inc susceptibility to infx, poor wound healing, hyperglycemia, inc. risk for osteoporosis, Cushing’s syndrome, potential adrenal suppression
First-line drug for juvenile arthritis
Methotrexate
Class: Methotrexate (MTX)
Anti-metabolite and anti-folate immunosuppressant and chemotherapeutic
MOA: Methotrexate (MTX)
Anti-metabolite, anti-folate drug
For cancer patients on Methotrexate (MTX), never give ___
folic acid
Class: Azathioprine (Imuran)
Purine anti-metabolite immunosuppressant
Indication: Azathioprine (Imuran)
Prevention of transplant rejection, IBD, SLE, RA
MOA: Azathioprine (Imuran)
Metabolic breakdown products of Azathioprine inhibit purine synthesis -> block protein synthesis
Class: Cyclosporine (Sandimmune)
Immunosuppressant (derived from soil fungus)
Indication: Cyclosporine (Sandimmune)
Prevent rejection of KD, LV, and heart transplants, RA, severe psoriasis
MOA: Cyclosporine (Sandimmune)
T-cell inhibition -> inhibition of IL-1, IL-2, IL-3, IL-4, IFN-gamma
Class: Tacrolimus (Prograf)
Immunosupressant (derived from soil microorganism)
Indication: Tacrolimus (Prograf)
Protection against rejection of organ transplantation
Topical for severe eczema
MOA: Tacrolimus (Prograf)
T-cell inhibition
100x more potent than Cyclosporine
Contraindications: Tacrolimus (Prograf), Cyclosporine (Sandimmune)
Use w/ grapefruit juice
Which immunosuppressant can be used in the eye to stimulate tear production?
Cyclosporine (Sandimmune) as Restasis
Class: Etanercept (Enbrel)
DMARD, recombinant-DNA drug
Indication: Etanercept (Enbrel)
Mod-sev RA, mod-sev. polyarticular juvenile arthritis, psoriatic arthritis, ankylosing spondylitis, mod-sev. plaque psoriasis
MOA: Etanercept (Enbrel)
Reduction of inflammation via anti-TNFalpha action
Class: Infliximab (Remicade)
DMARD, recombinant-DNA drug
Indication: Infliximab (Remicade)
RA, Crohn’s, UC
MOA: Infliximab (Remicade)
prevents binding of TNF-a with its receptors by binding to free TNF-a
MOA: Infliximab (Remicade) vs Etanercept (Enbrel)
Infliximab causes apoptosis of TNFa-expressing activated T-cells
Why infliximab has been used with success in Crohn’s and UC, while Etanercept has not
Which of the drugs used for RA or lupus is also used to treat malaria?
Hydroxychloroquine (Plaquenil)
MOA: Hydroxychloroquine (Plaquenil)
Blocks activation of TLRs on plamacytoid dendritic cells
Increases lysosomal pH
Class: Hydroxychloroquine (Plaquenil)
Immunosuppressant and anti-malarial
Indication: Hydroxychloroquine (Plaquenil)
RA, SLE, Sjogren’s, malaria
Side effects: Hydroxychloroquine (Plaquenil)
Corneal/macular damage, D, HA, N/V, hives, itching rash, loss of hair
Pts with G6PD deficiency: severe anemia
OD: drowsiness, HA, vision problems, SOB, convulsions
Which immunosuppressant requires regular ophthalmologic exams dt the possibility of corneal and macular damage?
Hydroxychloroquine (Plaquenil)
What is a last-option drug for RA?
Gold salts - Auranofin (Ridaura)
What is tachyphylaxis?
rapid decrease in the response to a drug over a relatively short period of time
Corticosteroids: Short-acting (8-12 hrs)
Hydrocortisone
Corticosteroids: Intermediate-acting (18-36 hrs)
Prednisone
Corticosteroids: Long-acting (24-72+ hrs)
Dexamathasone
Betamethasone
If hydrocortisone is considered a “1” for its anti-inflammatory effect, prednisone is a ___.
4
If hydrocortisone is considered a “1” for its anti-inflammatory effect, dexamethasone is a ___.
30
If hydrocortisone is considered a “1” for its anti-inflammatory effect, betamethasone is a ___.
35
Abrupt discontinuation of a glucocorticoid can result in ___, which can be lethal.
Acute adrenal insufficiency syndrome (Addisonian crisis)
SSx: Addisonian Crisis
Severe lethargy Severe V/D (dehydration) Low blood pressure Confusion Hyponatremia, hypoglycemia LOC Convulsions
Class: Prednisone (Deltasone)
Glucocorticoid (corticosteroid)
MOA: Prednisone (Deltasone)
Alters gene transcription
Class: Dexamethasone (Decadron)
Fluorinated corticosteroid
Indications: Dexamethasone (Decadron)
IV (intracranial pressure)
MOA: Dexamethasone (Decadron)
Affects gene transcription
Class: Triamcinolone inhaler (Azmacort)
Corticosteroid
Indications: Triamcinolone inhaler (Azmacort)
Asthma (not acute attack), COPD
MOA: Triamcinolone inhaler (Azmacort)
Dec. inflammation of bronchial wall
Affects gene transcription
Aldosterone is reduced in __ and increased in __.
Addison’s dz
Conn’s syndrome
Class: Fludrocortisone (Florinef)
Halogenated glucocorticoid (mineralcorticoid agonist)
Indications: Fludrocortisone (Florinef)
Mineralcorticoid replacement for pts w/ Addison’s dz and other cases of hyponatremia
MOA: Fludrocortisone (Florinef)
Na retention at renal tubular cells
Contraindications: Fludrocortisone (Florinef)
Not indicated as an anti-inflammatory agent
High potency corticosteroids (2)
Betamethasone
Dexamethasone
Medium potency corticosteroids (4)
Methylprednisolone
Triamcinolone
Prednisolone
Prednisone
Low potency corticosteroids (2)
Hydrocortisone
Cortisone
Mineralcorticoid activity (2)
Cortisone
Hydrocortisone
More Corticosteroid effect than Mineralcorticoid effect (2)
Prednisolone
Prednisone
No Mineralcorticoid activity (4)
Betamethasone
Dexamethasone
Methylprednisolone
Triamcinolone
DEA - Schedule I
No currently accepted medical use, high potential for abuse
DEA - Schedule II
High potential for abuse (less than schedule I)