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Pharmacology > Autacoids > Flashcards

Autacoids Flashcards

1
Q

H1 Receptors
Type
Location
Action

A
  • Gq-coupled. Nerves, smooth muscle, bronchi, intestines.
  • Causes vasodilation, capillary permeability (edema, hives), bronchoconstriction, pain, itch, and intestinal smooth muscle contraction.
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2
Q

H2 Receptors
Type
Location
Action

A
  • Gs-coupled. Gastric mucosa, heart, and mast cells.
  • Vasodilation, increased HR via reflex tachycardia (due to decreased baroreceptor firing following vasodilation) and direct stimulation, gastric acid secretion.
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3
Q

H3 Receptors
Type
Location
Action

A

Gi-coupled (inhibitory). Autoreceptors on histaminergic neurons.

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4
Q

H4 receptors
Type
Location

A

Gi-coupled. Eosinophils, neutrophils, CD4 T cells.

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5
Q 
Diphenhydramine
Brand Name
Generation
Receptor
Tx
Adverse Effects
Precautions
A

Benadryl, Sominex
• 1st generation. H1 inverse agonist
• Tx allergic rhinitis, sneezing, itching, urticaria, insomnia (produces sedation).
• Antimuscarinic (Ach) activity – treats motion sickness (NV, vertigo). Also has antiparkinsonian effects.
Adverse Effects
• CNS: confusion, dizziness, sedation
• Antimuscarinic effects: mydriasis (pupil dilation), xerostomia (dry mouth), reduced bronchial secretions, tachycardia, constipation, urinary retention
• Avoid in people w/ glaucoma due to mydriasis.
• Greatly metabolized by 2D6. Avoid in people w/ hepatic disease.

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6
Q 
Cetirizine
Brand Name
Generation
Receptor
Tx
Adverse Rxns
Precautions
A 
Zyrtec
2nd generation.  H1 inverse agonist.
•	Tx allergic conditions
•	Less sedating than 1st gen.
•	Minimal antimuscarinic activity
•	Few adverse rxns.  Xerostomia.
•	Do not exceed 5 mg / day if CrCL less than 31 mL / min.
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7
Q 
Fexofenadine
Brand Name
Generation
Receptor
Tx
Adverse Effects
Precautions
A 
Allegra
2nd generation.  H1 inverse agonist.
•	Tx allergic conditions
•	No antimuscarinic effects
•	Few adverse rxns.  
•	Avoid taking w/ fruit juices due to decreased absorption
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8
Q 
Loratadine
Brand Name
Generation
Receptor
Tx
Adverse Effects
A 
Claritin
 2nd generation.  H1 inverse agonist.
•	Tx allergic conditions
•	Little / no antimuscarinic activity
•	Few adverse rxns.
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9
Q

Cimetidine
Receptor
Tx
Adverse Effects

A

H2 inverse agonist
• Tx for peptic ulcer disease, GERD, and dyspepsia (indigestion)
• May cause moderate / severe headaches and rare blood dyscrasia (neutropenia, leukopenia, etc)

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10
Q 
Ergotamine
Receptor
Mechanism
Tx
Adverse Rxns
Precautions
A

Serotonin partial agonist / antagonist. Causes vasoconstriction.
• Tx migraines
• Oxytocic agent → uterine contractions. Decreases postpartum bleeding via constriction.
• Metabolized by 3A4
Adverse rxns: NVD, xerostomia
• Ergotism: angina, asthenia, coronary vasospasm, cramps, myalgia, paresthesias, changes in HR; vasoconstriction may result in hypothermia or tissue necrosis
Precautions – avoid when vasoconstriction would cause problems
• CV: angina, arteriosclerosis, coronary artery disease, hypertension, peripheral vascular disease, Raynaud’s disease, thrombophlebitis, MI, stroke
• Hepatic disease, biliary tract disease, cholestasis
• Renal failure or impairment
• FDA Pregnancy Risk Category X (due to labor induction)

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11
Q 
Sumatriptan
Receptor
Tx
Adverse Rxns
Precautions
A

Agonist at 5HT-1D autoreceptors (system inhibition) and 5HT-1B → vasoconstriction
• Tx migraines. Not for prophylaxis.
Adverse rxns
• Fatal CV events (coronary artery vasospasm, arrhythmias, MI)
• GI: NVD, vasospasm → bowel ischemia, abdominal pain, bloody diarrhea
Precautions – again, sxs that vasoconstriction would exacerbate.
• CV: angina, arteriosclerosis, arrhythmias, coronary artery disease, hypertension, peripheral vascular disease, Raynaud’s disease, thrombophlebitis, MI, stroke; evaluate CV function before prescribing
• Ischemic bowel disease

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12
Q

Thromboxane (TXA2)

A

Vasoconstriction and platelet aggregation. TP receptors.

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13
Q

Prostacyclin (PGI2)

A

Vasodilation and inhibited platelet aggregation. Physical antagonist of thromboxane. IP receptors.

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14
Q

PGD2

A

Smooth muscle contraction and inhibited platelet aggregation. DP receptors.

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15
Q

PGE2

A

Vasodilation, pain, fever, diuresis, immunomodulation. EP receptors.

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16
Q

PGF-a

A

Smooth muscle contraction: vasoconstriction, bronchoconstriction, uterine contraction. FP receptors.

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17
Q 
LTB4
Released by
Target
Action
Receptors
A

Released by and acts on neutrophils (autoregulation). → plasma exudation. BLT1 and BLT2 receptors.

18
Q 
Cysteinyl Leukotrienes
Types
Released by
Action
Receptors
A

Include LTC4, LTD4, and LTE4 – released by mast cells, basophils, and eosinophils. → bronchoconstriction, vasoconstriction, decreased blood flow, decreased contractility, and plasma exudation. CysLT1 and CysLT2 receptors.

19
Q

Lipoxins
Types
Receptor
Action

A

LXA4 and LXB4 bind ALX receptors. Antagonize effects of leukotrienes (cause relaxation). Competitively inhibit CysLT1 receptors.

20
Q

Systemic effects of cortisol

A

Stimulates GNG, immunosuppressive / anti-inflammatory effects. Also increased blood glucose and insulin, lipolysis and lipogenesis, stimulates protein / bone catabolism

21
Q

Anti-inflammatory effects of corticosteroids
Increases?
Decreases?

A
  • Increases: annexin 1 (inhibits PLA2), SLPI (secretory leukoprotease inhibitor), IL-10 (inhibits cytokines), and NFkB-inhibitor (nuclear factor kB, activates immune system).
  • Decreases: COX-2, cytokines (IL-1, 2), chemokines (IL-8), CAMs, inflammatory enzymes
22
Q 
Hydrocortisone
Action
Tx
Adverse Effects
Precautions
A

Natural steroid hormone. Inhibits COX-2 expression, decreases cytokines, induces apoptosis of eosinophils.
• Tx anti-inflammatory: anaphylaxis, asthma, COPD, IBD, rheumatism, dermatoses
• DOC for glucocorticoid replacement therapy
• No adverse rxns w/ acute use. Prolonged use may result in dependence due to HPA suppression → hyperglycemia, immunosuppression, cataracts, glaucoma
• Precautions – abrupt DC of prolonged systemic therapy and Cushing’s Syndrome

23
Q 
Prednisone
Action
Tx
Metabolism
Adverse Rxns
Precautions
A

Represses COX-2 expression, decreases cytokines, apoptosis of eosinophils
• Tx for autoimmune disorders (asthma, IBD, rheumatoid) and allograft rejection
• Prodrug of prenisolone (active)
Adverse Rxns
• CNS: headache, insomnia, vertigo, depression, anxiety, euphoria, personality changes, psychosis
• GI: NVD, anorexia, gastritis
• Cataracts
• Opportunistic infections (thrush, fungal infection in oral cavity due to immunosuppresion)
Precautions – Cushing’s, abrupt DC of prolonged therapy, cataracts

24
Q 
Fluticasone
Mechanism
Tx
Adverse effects
Precautions
A

Medium potency – same mechanism as others.
• Tx for dermatoses (psoriasis), allergic / nonallergic rhinitis, and asthma prevention only.
• Adverse effects: pruritis, burning, hypertrichosis (hair overgrowth), hoarseness, irritation, 2ndary infections (thrush)
• Precautions – Cushing’s, avoid DC for prolonged use, cataracts

25
Q

Dexamethasone

A

Corticosteroid
Very strong anti-inflammatory effects.
Long duration

26
Q 
Aspirin
Brand Name
Action
Tx
Adverse Rnxs
Precautions
A

Bayer
Irreversible COX inhibitor. 5x selective for COX-1
• Tx for thrombosis prevention – reduces risk of MI, stroke, TIA, etc. Other general NSAID actions as well.
• Antiplatelet effect lasts 8-10 days b/c new platelets have to be made.
• Metabolized in liver to salicylic acid
Adverse Rxns
• GI disturbances (2-30%): NVD, mucosal damage, bleeding, pain
• Tinnitus or hearing loss with high doses
• Hypersensitivity and anaphylactic reactions in pxs w/ chronic urticaria (20%), asthma (4%), or chronic rhinitis (1.5%)
• Sensitivity manifests as bronchospasm in asthmatics and is commonly associated with nasal polyps
• Aspirin Triad – aspirin hypersensitivity, asthma, and nasal polyps
• Precautions – Children Reye’s syndrome), renal disease, bleeding disorders

27
Q 
Ketorolac
Action
Tx
Adverse Rxns
Precautions
A

Competitive inhibitor of COX. 100x selective for COX-1.
• Short-term use as strong analgesic (opioid level) following surgery
• 90% excretion in urine
Adverse rxns:
• CNS: headaches, dizziness, drowsiness
• GI: NVD, mucosal damage, gastric bleeding, abdominal pain
• Precautions – salicylate sensitivity, aspirin triad, CrCL less than 30 mL / min

28
Q 
Indomethacin
Action
Tx
Adverse Rxns
Precautions
A

Competitive inhibitor of COX. 3-5x selective for COX-1.
• Accelerates closure of ductus arteriosus in premature infants. Duct normally maintained by prostaglandins, which decrease after normal birth.
• Other normal anti-inflammatory effects.
• Indole group may effect serotonin → CNS problems
Adverse rxns:
• CNS: headache (>10%), dizziness, fatigue, depression, tremor, ataxia
• GI: VND, mucoal damage, etc.
• Precautions – salicylate sensitivity, aspirin triad, CNS disorders, Pregnancy Risk Category D in 3rd trimester

29
Q 
Naproxen
Brand Name
Action
Tx
Adverse Rxns
Precautions
A

Aleve
Competitive inhibitor of COX. 3-5x selective for COX-1.
• Better for lower back pain that other NSAIDs.
• Long duration of action due to long half-life
Adverse Effects
• GI: risk of upper GI bleeding is double that of OTC ibuprofen
• DERM: rashes, urticaria, alopecia (hair loss)
Precautions: salicylate sensitivity, aspirin triad

30
Q 
Meloxicam
Action
Tx
Adverse Rxns
Precautions
A

Competitive inhibitor of COX. 10x selective for COX-2.
• Used for Rheumatoid and osteoarthritis
• Good choice if px needs chronic NSAID use (due to COX-2 selectivity)
• Adverse Rxns: GI (pain, dyspepsia, nausea)
• Precautions: salicylate sensitivity, aspirin triad, normal others

31
Q 
Celecoxib
Brand Name
Action
Adverse Rxns
Precautions
A

Celebrex
Competitive inhibitor of COX. 10-20x selective for COX-2.
• First FDA-approved selective COX-2 inhibitor.
• Adverse Rxns: GI, dizziness, rash
• Precautions: same as others

32
Q 
Diclofenac
Action
Metabolism
Adverse Rxns
Precautions
A

Competitive inhibitor of COX. 10-20x selective for COX-2.
• Metabolized by CYP2C9 followed by glucuronidation / sulfation
Adverse rxns
• GI: upset stomach, heartburn, bleeding, ulceration, perforation, elevated LFTs
• Renal: decreased blood flow and GFR. If balance is shifted toward thromboxane, vasoconstriction may occur → renal damage.
• Precautions – same as others. Mainly focus on hepatic disease.

33
Q 
Acetaminophen
Brand Name
Action
Tx
Limit
Metabolism
Antidote
Adverse Rxns
Precautions
A

Tylenol
Competitive COX inhibitor (only in CNS). Binds to cannabinoid receptors in spinal cord.
• Analgesic and antipyretic, but NO anti-inflammatory / platelet effects
• Good for pxs who can’t use aspirin (pxs w/ clotting disorders or triad)
• Do not exceed 4g / day
• Metabolized by liver. Most undergoes glucuronidation or sulfation, but 10-15% converted to reactive hepatotoxic metabolites by CYP enzymes. Intermediates react w/ sylfydryls → protein interaction → cell death.
• Antidote is N-acetyl cysteine, which has sulfhydryls and acts as “decoy” to prevent toxic intermediates from forming.
Adverse rxns
• Skin: rash, pruritis, urticaria
• GI disturbances (high dose): NV, anorexia, and abdominal pain usually occur within 2-3 hr after ingestion of toxic doses
• Hepatotoxicity; in acute overdose, 2-3 days pass before maximum liver damage becomes apparent.
• Renal tubule necrosis with high or chronic doses
• Precautions: alcoholism, hepatic disease, renal disease, tobacco smoking (CYP inducer → more reactive metabolites), salicylate sensitivity

34
Q 
Alprostadil
Action
Tx
Adverse Rxns
Precautions
A

Synthetic PGE1. Agonist at EP receptors → cAMP → vasodilation
• Tx for erectile dysfunction (EP receptors for ED) and maintains patency of ductus arteriosus
• Injected into penis
Adverse rxns
• ED: penile pain, prolonged erection, penile fibrosis
• PEDS: fever, apnea, flushing
Precautions – follow up w/ penis exam, use lowest possible dose w/ infants

35
Q 
Latanoprost
Action
Tx
Metabolism
Adverse Effects
Precautions
A

Synthetic PGF2a. Agonist at FP receptor
• Tx reduces elevated IOP in pxs w/ open-angle glaucoma. Increases outflow.
• Prodrug – esterases in cornea hydrolyze to active form.
• Adverse effects: blurred vision, burning, itching, increased iris pigmentation (melanin), thicker eyelashes.
• Precautions – intraocular inflammation, remove contacts for 15 min

36
Q 
Zileuton
Action / Types
Tx
Metabolism
Adverse Effects
Precautions
A

5-LOX inhibitor (decreases LTB4, LTC4, LTD4, and LTE4). Inhibits leukocyte migration, aggregation, adhesion, capillary permeability, and smooth muscle contractions
• Used for prophylaxis asthma treatment (NOT bronchodilator)
• Substrate for 1A2, 2C9, and 3A4.
• Adverse Rxns: dyspepsia, elevated LFTs
• Precautions – liver disease (do LFTs before and after tx), alcoholism, smoking, age

37
Q 
Zafirlukast
Action
Tx
Adverse Effects
Precautions
A

Antagonist at G protein cysteinyl leukotriene receptors (CysLT1) in airway smooth muscle, mast cells, and neutrophils.
• Prophylaxis of asthma (NOT bronchodilator). Inhibits bronchoconstriction, edema, and mucous.
• Metabolized by 3A4 and 2C9
• Few adverse rxns. Rare elevated LFTs.
• Precautions – hepatic disease

38
Q 
Montelukast
Action
Tx
Excretion
Adverse Rxns
Precautions
A

CysLT1 antagonist in airway smooth muscle, mast cells, neutrophils
• Tx allergic rhinitis and asthma prophylaxis (NOT bronchodilator). Inhibits bronchoconstriction, edema, and mucous secretion
• 3A4 and 2C9 metabolism. Excreted through bile.
• Few adverse rxns
• Precautions – liver disease, alcoholism, smoking, age
• Person w/ impaired renal function might be better off w/ montelukast than zafirlukast

39
Q

Ibuprofin
Action
Adverse Rxns
Precautions

A

Competitive inhibitor of COX. 2x selective for COX-1.
Adverse Rxns:
CNS - dizziness, heachache, nervousness
GI - NVD, damage to mucosa, gastric bleeding, abdominal pain
Rash
Tinnitus
Blurred vision
Precautions: salicylate sensitivity, aspirin triad, normal others (heart, hepatic, GI bleeding, bleeding disorders.

40
Q 
Misoprostol
Action
Tx
Adverse Effects
Precautions
A

Agonist at EP receptors on parietal cells –> low cAMP –> decreases stomach acid secretion AND increases mucous / bicarb production. 2 fold.
Tx for gastric ulcers. Not as effective as H2 antagonists. May be used to counteract stomach bleeding w/ NSAIDS.
Also induces PG termination ( contractions and dilates cervix. Labor induction.
Adverse Effects: headache, diarrhea, pain, NV
Precautions: pregnancy risk category X

Pharmacology (6 decks)

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