Pharmacology Flashcards by Stephen Jensen

Describe the rational use, MOA, site(s) of action, and adverse effects of Pilocarpine (Pilopine).

Uses: treats Glaucoma.
MOA: Direct acting Cholinergic Stimulant.
Sites of Action: Muscarninic/Nicotinic rectors.
Adverse effects: MUBBLEDSS (Miosis, Urination, Bradycardia, Bronchoconstriction, Lacrimation, Excitation of CNS, Diarrhea, Salivation, Sweating)

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Describe the rational use, MOA, site(s) of action, and adverse effects of Physotigmine and Organophosphates.

Uses: Treat glaucoma. Atropine antidote.
MOA: Reversible, Indirect acting Cholinergic stimulant. Inhibits Acetylcholinesterase.
Uses: Glaucoma, Insecticides, Nerve gas.
MOA: Irreversible, Indirect acting Cholinergic stimulant. Inhibits Acetylcholinesterase.

-Adverse effects: MUBBLEDSS (Miosis, Urination, Bradycardia, Bronchoconstriction, Lacrimation, Excitation of CNS, Diarrhea, Salivation, Sweating)

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Describe the rational use, MOA, site(s) of action, and adverse effects of Atropine.

Uses: Dilate pupils
MOA: Antimuscarinic Cholinergic antagnoist. Blocks muscarinic receptors.
Adverse affects of Anticholinergics: Dry mouth, Blurred vision, Urinary retention, Constipation, Tachycardia, Sedation, Hallucination.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Antinicotinic drugs (autonomic ganglion blockers and neuromuscular junction blockers.

MOA: Cholinergic antagonists. Block Nictonic receptors.

Autonomic ganglion blockers. N2. Used for emergent HTN.
Neuromuscular junction blockers. N1. Relax skeletal muscle during surgery.
Adverse effects: Dry mouth, Blurred vision, Urinary retention, Constipation, Tachycardia, Sedation, Hallucination.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Phenylephrine.

Uses: Treats nasal congestion.
MOA: a-1 selective adrenergic agonist. Causes vasoconstriction.
Adverse effects: HTN, headache, reflex bradycardia.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Clonidine (Catapres)

Uses: treat HTN.
MOA: a-2 selective agonist.
Adverse effects: dizziness, drowsiness, dry mouth.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Isoproterenol.

Uses: Treat bronchospasm and some cardiac arrythmias.
MOA: Non-selective beta adrenergic agnoist. Binds both B1 and B2 receptors.
Adverse effects: Cardiac Diagnoses warning! Be careful prescribing this for bronchospasm if they have cardiac issues.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Dobutamine.

Uses: Treats shock, heart failure. (lots of B1 receptors in cardiac tissues).
MOA: B1 selective adrenergic agonist.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Albuterol (Proventil).

Uses: Treat pulmonary diseases with decreased pulmonary diameters.
MOA: B2 selective adrenergic agonist.
Adverse effects: nervousness/restlessness.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Epinephrine (Epipen).

Uses: Tx of anaphylactic shock, asthma, hypotension.
MOA: Mixed alpha and Beta adrenergic agonists.
Adverse effects: excess CNS excitation, excess stimulation of CVS.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Prazosin (Minipres).

Uses: Tx of HTN, BPH.
MOA: alpha 1 selective adrenergic antagonist.
Adverse effects: bronchoconstriction, excess decreased cardiac function.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Propranolol (Inderal).

Uses: Treats cardiac conditions.
MOA: Non-selective B adrenergic antagonists.
Adverse effects: bronchoconstriction, excess decreased cardiac function.

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Describe the rational use, MOA, site(s) of action, and adverse effects of Metoprolol (Lopressor).

Uses: Cardiac conditions. Fewer side effects in those who also have pulmonary Dx.
MOA: B1 selective adrenergic antagonist.

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Know the MOA, side effects, and ADME for Salmeterol, Formoterol.

LABA

b. MOA: Decrease number of attacks in mild-moderate asthma. Stimulate B2 Adrenergic receptors in same fashion as SABA’s but last longer. Often used in combination with glucocorticoids or other bronchodilators.
c. Side Effects: Muscle tremor, Tachycardia, Metabolic effects with large systemic administration (increased FA, insulin, and glucose), Hypokalemia, Paradoxical bronchospasms (rare, exacerbates issue).
d. ADME: High lipid solubility causes them to be trapped in PM and have slower kinetics.

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Know the MOA, side effects, and ADME for Albuterol, Levalbuterol, Terbutaline, Metaproterenol

SABA

b. MOA: Inhalers used for immediate relief of bronchoconstriction by stimulating B2 Adrenergic receptors. Increase intracellular cyclic AMP levels. Decrease intercellular calcium levels. Inhibit mosin light chain kinase activation. Stimulate potassium channel to hyperpolarize membrane.
c. Side Effects: Muscle tremor, Tachycardia, Metabolic effects with large systemic administration (increased FA, insulin, and glucose), Hypokalemia, Paradoxical bronchospasms (rare, exacerbates issue).
d. ADME: Inhaled for immediate response.

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Know the MOA, side effects, and ADME for Fluticasone , Budesonide, Beclomethasone dipropionate, Ciclesonide

ICS

c. MOA: Mimic Coritsol.
(1) Promote synthesis of lipocortins→ Inhibits synthesis of leukotrienes and prostaglandins by blocking A2/production of Arachidonic acid.
(2) Decrease acetylation of specific genes→ DNA more tightly wound→ ↓ Gene Expression. (Not helpful in COPD due to altered DNA cetylation in COPD).
(3) Can increase response to β2 agonists→ Synergistic effects so often used with LABAs.
d. Side Effects:
(1) Local (suppressing immune system in mouth and throat): Dysphonia, Thrush, Cough
(2) Systemic: Adrenal suppression, Growth suppression, Bruising, Osteoporosis, Cataracts, Glaucoma, Metabolic abnormalities, Psychiatric imbalance, Pnemonia.
e. ADME: Inhaled to minimze systemic effects from necessarily high concentrations.

Know the MOA, side effects, and ADME for : Ipratropium, Tiotropium

Anticholinergics (Muscarininc Antagonists)

b. MOA: 2nd line agent for patients that can’t tolerate B2 agonists in high doses. Good for COPD.
c. Side Effects: Minor rebound effect, Glaucoma in elderly.

Know the MOA, side effects, and ADME for Montelukast, Zafirlukast

Leukotriene antagonist
i MOA: Leukotriene receptor (CysTL1 inhibitor). Prophylactic, not reversal of bronchospasm attack.
ii ADME: Good for aspirin indueced asthma. Can be taken as pill.

Know the MOA, side effects, and ADME for Zileuton

Leukotriene antagonist
i MOA: iron chelator that interferes with 5-lioxygenase enzyme and blocks synthesis of leukotriens. Prophylactic, not reversal of bronchospasm attack.
ii Side Effects: liver toxicity.
iii ADME: Poor affinity therefore must use high concenration. Short half-life therefore must take multiple times per day.

Know the MOA, side effects, and ADME for Theophylline, Roflumilast (PDE4)

Methylxanthines

b. MOA: Acts by multiple mechanisms to cause bronchodilation, blocks adenosine receptor. Given to pateitns who don’t respond to 1st line drugs. Roflumilast is selective PDE4 inhibitor.
c. Side Effects: Flutter, tachycardia, Irritability and reselssness, Seizures, Diarrhea, N/V, Tremor, Diuresis.
d. ADME: Cannot be administered by inhaler.

Know the MOA, side effects, and ADME for Cromolyn sodium

Release Inhibitor (Mast Cell Stabilizer

b. MOA: Prophylactic. Can’t reverse bronchospasms.
c. Side Effects: Dry mouth, Cough, Throat irritation.
d. ADME: Must be inhaled as aerosol(insoluble salt). Short half life must take 2-4 times per day.

Know the MOA, side effects, and ADME for Prednisone, Hydrocortisone

Systemic Corticosteroids

b. MOA: Act as Cortisol. Inibit inflammation.
c. Side Effects:
d. ADME: Used for severe asthma attacks that can’t be controlled with ICS or bronchodilators.

Know the MOA, side effects, and ADME for Omalizumab

Immunomodulator

b. MOA: Reduces hypersensitivity of the airways. Used for chronic severe asthma unresponsive to high [ICS] with demonstrated IgE-mediated sensitivity.
c. Side Effects: Injection site reactions, Infections, Allergic reactions.
d. ADME: SubQ injection. Slow absoption. Mostly cleared through the liver.

Know the use, MOA, and ADME for Hydroxyurea.

Treatment for sickle cell anemia.
MOA: blocks ribonucleotide reductase
Adverse: bone marrow suppression, teratogen in pregnancy.

Know the use and MOA for Thrombopoietin.

- Stimulates megakaryopoiesis. Increases platelet counts in ITP and cancer chemotherapy. - MOA: Growth factor, romiplostim peptide copies bind thrombopoietin receptor.

Know the name use, MOA, and side effects of IL-11

- IL-11 Oprelvekin - Use: non myeloid cancers with severe thrombocytopenia - MOA: Growth factor, Enhances megakaryocyte maturation. - Causes edema.

Know the use and MOA of G-CSF (filgrastim)

- Use: After bone marrow transplant, cancer chemotherapy | - MOA: stimulates neutrophil production

Know the uses, and MOA of GM-CSF (sargramostim)

- Uses: bone marrow transplant to shorten neutropenia, Blood stem cell collection, chemo adjuvant. - MOA: growth factor, stimulates myelopoeisis

Know the uses, supplementation, MOA, and adverse effects of erythropoietin.

- Uses; anemia due to CKD. - Fe and Folate supplementation - MOA: stim RBC production - Side effects: HTN, thrombotic events

Know the uses, MOA, ADME, adverse effects for Chloroquine

-Uses: Anti-malarial -MOA: Blood schizonticide; concentrates in vacuoles preventing proper heme breakdown. Buildup of free heme is toxic to parasite -ADME: Oral (rapid and complete absorption); Large VD; 3-5 day initial half-life, long terminal half-life (1-2 months) - Adverse effects: Well tolerated, pruritus somewhat common in Africans Large list of rare events, so always have pts inform you of any adverse drug reactions (*vivid dreams, nightmares)

Know the uses, MOA, ADME, adverse effects for Atovaquone-proguanil (Malarone)

- Uses: Anti-malarial - MOA: Disrupts mitochondrial electron transport. Active against both liver tissue and blood schizonts, so can discontinue at one week post exposure - ADME: Oral (poor absorption - eat with fatty foods); Eliminated unchanged in feces; Half life 2-3 days - Adverse effects: Well tolerated, but some GI effects, headache, rash Alone, only marginally effective due to fast development of resistance. Highly effective in combo with proguanil

Know the uses, MOA, ADME, adverse effects for Proguanil

- Uses: Anti-malarial - MOA: DHFR (dihydrafalate reductase) inhibitor, only effective against erythrocytic forms - ADME: Given as a prodrug, active form is cycloquanil. Reasonable absorption, 16hr half life. - Adverse effects: well tolerated. * Contraindicated in pregnancy (mothers need to take Folic Acid to prevent neural defects)

Know the uses, MOA, ADME, adverse effects for Mefloquine

-Uses: anti-malarial - MOA: Unknown, effective against erythrocytic forms -ADME: Only oral, 20 day half life (dose weekly) -Adverse Effects: Higher than other drugs GI effects, behavioral disturbances, dizziness, sedation, seizures (don't give to epileptic or psychotic patients). Vivid dreams

Know the uses, MOA, ADME, adverse effects for Primaquine

Anti-malarial -MOA: Unknown. DOC for eradication of dormant liver forms of vivax and ovale. Active against hepatic, dormant, and gamete stages, not against erythrocytic stage. -ADME: Oral (good absorption); 3-8 hr half-life. Rapid metabolism and excretion in urine -Adverse effects: Well tolerated GI effects, but less when taken with food. One of its metabolites is implicated in hemolysis. Exacerbates G6-PD deficiency.

Two major malarial treatment regimens when Chloroquine (prophylaxis) isn't effective

Atovaquone-proguanil (Malarone) | Artemether-lumefantrine (Coartem)

Know the uses, MOA, ADME, adverse effects for Artemether-lumefantrine (Coartem)

Uses: treatment of malaria -MOA: Converted into free radicals in the parasite food vacuole, and a Ca ATPase inhibitor. Good against erythrocytic forms (blood schizonticide) -ADME: oral or parenteral, 1-3 hour half-life -Adverse effects: Well tolerated GI effects, dizziness

Lumefantrine

Uses: treatment of malaria -MOA: Unsure, but possibly inhibits formation of beta-hematin (storage structure that parasite uses to get rid of high levels of heme inside parasite) [hemozoin] -ADME: oral with food. Some CYP3A4 metabolism - Adverse effects: Well tolerated GI effects, some prolongation of QT interval (Increases chance of arrythmia)

Tetracyclines

Uses: treatment of malaria (?) -MOA: Competitively blocks binding of tRNA to A site of 30S subunit, preventing addition of new amino acids to the growing peptide chaine -Administration: Oral (variable bioavailability - 30-100%); IV (only for Tigecycline) - Half life: Short - 6-8 hours (tetracline); Intermediate - 12 hours; Long- 16-18 hours (doxycycline, minocycline) -Adverse effects: Discoloration of teeth and hypoplasia of enamel in children under 8 y.o. (b/c tetracylines are concentrated in growing teeth and bone) Should not be used in pregnant women after 4th month of gestation (avoid discoloration in fetus) Cause phototoxicity (abnormal sunburn) Divalent cations block absorption, ask about supplements. * Must be discarded at expiration date due to slow degradation of tetracycline to toxic compounds * Type IV hypersensitivity

Doxycycline?

On list of drugs to know in objectives, but no info in slides?