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Cardiovascular drugs – Part 1 DHP CCB: MOA = blocks Ca2+ channel in cardiac tissue + smooth muscle in BV = increased vasodilation + decreased peripheral resistance Nifedipine (Procardia, Adalat CC, Nifedical XL): Felodipine (Plendil): Common uses: hypertension chronic stable + variant angina...

Cardiovascular drugs – Part 1 DHP CCB: MOA = blocks Ca2+ channel in cardiac tissue + smooth muscle in BV = increased vasodilation + decreased peripheral resistance Nifedipine (Procardia, Adalat CC, Nifedical XL): Felodipine (Plendil): Common uses: hypertension chronic stable + variant angina SE: hypotension => reflex tachycardia vasodilation gingival hyperplasia (practice good dental hygiene) increase dose = worsen angina/ risk of MI avoid grapefruit/ juice do not discontinue abruptly extended release - empty stomach Common uses: Hypertension SE: hypotension => reflex tachycardia Vasodilation Gingival hyperplasia Increased dose = worsens angina/risk for MI Avoid grapefruit/juice Do not discontinue abruptly Non-DHP CCB: increased vasodilation + decreased peripheral resistance + decreased force of contraction + decreased heart rate. Diltiazem (Cardizem, Cartia XT, Dilacor XR, Tiazac): Verapamil (Calan, Verelan): Common uses: Hypertension Arrythmia in atria Tachycardia Chronic stable angina SE: Peripheral edema Headache Dizzy Bradycardia CONTRAINDICATION: 2nd/3rd AV block + severe left ventricular dysfunction Substrate/Inhibitor for CYP3A4 Do not discontinue abruptly Common uses: Hypertension Arrythmia in atria Tachycardia Chronic stable, unstable, variant angina SE: peripheral edema Headache Dizzy Bradycardia Constipation CONTRAINDICATION: 2nd/3rd AV block + severe left ventricular dysfunction Substrate/Inhibitor for CYP3A4 Do not discontinue abruptly Alpha 1 blockers: vasodilation, pupil constriction, lack of urinary retention? Lack of ejaculation? Beta 1/2 blockers: decreased heart rate & contraction, less renin released so less sodium and water retained. Non-specific adrenergic blockers: B1/B2 blockers + A1 blockers: vasodilation of BV, CO reduced. Carvedilol (Coreg): Labetalol (Normodyne, Trandate): Common uses: Hypertension Heart failure MI => Left ventricular dysfunction SE: Hypotension Hyperglycemia Dizzy Fatigue CONTRAINDICATIONS: bronchial asthma (med can cause more bronchoconstriction – more parasympathetic) – 2nd or 3rd degree AV block – heart failure – severe bradycardia Do not discontinue abruptly. Take w/ food to decrease orthostatic hypotension. Common uses: Hypertension SE: Hypotension Dizzy Fatigue CONTRAINDICATIONS: bronchial asthma (med can cause more bronchoconstriction – more parasympathetic) – 2nd or 3rd degree AV block – heart failure – severe bradycardia Do not discontinue abruptly. Used to treat chronic hypertension in pregnancy B1/B2 blocker (more than specific): Propranolol (Inderal XL/LA, InnoPran XL): Common uses: Hypertension Chronic angina pectoris Essential tremor Migraine MI SE: diarrhea Dizzy Vomiting Fatigue BBW: Do not discontinue abruptly => angina, MI, arrythmia, rebound hypertension CONTRAINDICATIONS: bronchial asthma - 2nd or 3rd degree AV block – cardiogenic shock – severe sinus bradycardia Extended release = take w/ or w/o food (BE CONSISTENT) Immediate release = take w/ food B1 blocker (most selective): Metoprolol (Lopressor – metoprolol tartrate, Toprol X – metoprolol succinate) Nebivolol (Bystolic): Nitric oxide (NO) mediated vasodilation Atenolol (Tenormin): Common uses: Hypertension Chronic angina pectoris Acute MI (tartrate) Congestive heart failure (succinate) SE: Hypotension Hyperglycemia WHY? IDK Dizzy Fatigue BBW: Do not discontinue abruptly => angina, MI, arrythmia, rebound hypertension CONTRAINDICATIONS: AV block – bradycardia – cardiogenic shock – overt heart failure *mask symptom of hypoglycemia Take w/ food to increase absorption Common uses: Hypertension SE: Dizzy Headache Fatigue Nausea BBW: Do not discontinue abruptly => angina, MI, arrythmia, rebound hypertension CONTRAINDICATIONS: AV block – bradycardia – cardiogenic shock – overt heart failure *mask symptom of hypoglycemia Take w/ food to increase absorption Common uses: Hypertension Chronic angina pectoris Acute MI SE: Bradycardia Hypotension Dizzy Fatigue BBW: Do not discontinue abruptly => angina, MI, arrythmia, rebound hypertension CONTRAINDICATIONS: AV block – bradycardia – cardiogenic shock – overt heart failure *mask symptom of hypoglycemia Take w/ food to increase absorption Vasodilator: relaxes vascular smooth muscle Hydralazine (Apresoline): Common uses: Hypertension SE: Headache Palpitation Tachycardia Angina pectoris *may cause drug induced lupus erythematosus (DILE) – serum sickness – hemolytic anemia – vasculitis – glomerulonephritis Do CBC count and ANA titer before and during therapy. Possible risk for peripheral neuropathy [Add pyridoxine to regimen] Take w/ food to increase bioavailability [BE CONSISTENT] Antianginal: reduces intracellular Na+ levels and Ca2+ influx = less depolarization Ranolazine (Ranexa): Common uses: Chronic angina SE: Dizzy Headache Nausea Constipation CONTRAINDICATION: Don’t take w/ strong CYP3A4 inhibitors/inducers [max dose = 500mg bid when taken with CYP3A4 inhibitor] Avoid grapefruit/juice. May cause QT prolongation Antianginal/Vasodilator: PRODRUG for nitric oxide => relaxes vascular smooth muscle + dilation of peripheral veins & arteries Isosorbide Mononitrate (Imdur): Common uses: Angina pectoris (caused by coronary artery disease) SE: Headache Dizzy Lightheadedness Flushing DON’T use to treat acute anginal attacks {ONSET OF ACTION is not rapid enough} DON’T use w/ PDE-5 inhibitor (risk of severe hypotension) Immediate release: administered BID (7 hours apart to prevent tolerance) Extended release: can be divided in half Antiarrhythmic: blocks K/Na/Ca channel OR B-blocker Amiodarone (Cordarone, Pacerone) Propafenone (Rythmol): Digoxin (Digitek, Digox, Lanoxin): Class: blocks K channel Common use: ventricular arrythmia SE: Hypotension Heart block Pulm fibrosis Sinus bradycardia Skin discoloration Hypothyroidism Corneal deposit BBW: risk of pulm. toxicity, hepatotoxicity – worsened arrythmia *Monitor pulm. fn, thyroid fn, liver fn – Perform ophthalmic exam. Avoid St. John’s wort and grapefruit juice Class: blocks Na channel Common use: ventricular arrythmia Systemic Atrial fibrillation (AFib) SE: Dizzy Palpitations Chest pain Edema Taste disturbance BBW: proarrhythmic potential Major CYP2D6 subtrate Class: blocks NaK ATP-ase pump (increased contraction) + stimulates parasympathetic response (slows heart rate) Common use: Heart failure AFib SE: Diarrhea Nausea Vomiting Dizzy *Reduce dose in renal impairment (by 20-25%) Risk of toxicity in pt. with hypokalemia, hypomagnesemia, hypercalcemia Patients should report symptoms of toxicity. Cardiovascular drugs – Part 2 *This section completed in notability. Asthma = acute attack – chronic inflammation How to treat? B2 agonist (rescue inhaler) / Corticosteroid (maintenance inhaler) / Combo COPD = gradual lung destruction - Emphysema + Bronchitis How to treat? Long-acting agent (B2 agonist / anticholinergic / Combo) = Both opens airways slowly and keep open longer Metered Dose Inhaler (MDI) Dry Powder Inhalers (DPI) Brand name: HFA Dose delivery: aerosolized liquid Use propellant. Shake before use Immune drugs – Part 1 {CORTICOSTEROIDS} Topical steroids: anti-inflammatory agents – MOA: phospholipase A2 inhibitory proteins stimulated => release of arachidonic acid blocked which means leukotrienes and prostaglandin (inflammatory response) are not produced Clobetasol (Clobex, Olux, Temovate): Desonide (DesOwn, Desonate, Verdeso): Fluocinonide (Lidex, Vanos): Hydrocortisone (Westcort, Locoid): Triamcinolone (Kenalog): *dental paste Common uses: inflammatory and pruritic dermatoses (dry, itchy skin) SE: pruritis Burning sensation HPA suppression Monitor: response to treatment – ocular changes – HPA suppression with long use *Apply sparingly. Wash hands after application Avoid contact with face, axillae, groin. Do not cover with bandages/wraps/dressing. Do not use for more than 2 consecutive weeks – can cause skin thinning + striae (stretch marks) Common uses: inflammatory and pruritic dermatoses (dry, itchy skin); atopic dermatitis SE: pruritis Burning sensation HPA suppression Monitor: response to treatment – ocular changes – HPA suppression with long use – sign of bacterial/fungal infection. *Apply sparingly. Wash hands after application Do not cover with bandages/wraps/dressing. Do not use for more than 4 consecutive weeks – can cause skin thinning + striae (stretch marks) Common uses: inflammatory and pruritic dermatoses (dry, itchy skin) SE: pruritis Burning sensation HPA suppression Monitor: response to treatment –– HPA suppression with long use – sign of bacterial/fungal infection. *Apply sparingly. Wash hands after application Don’t use high strength 0.1% fluocinonide on face, groin, or axillae. Do not cover with bandages/wraps/dressing. No improvement in 2 weeks = contact prescriber Overuse = skin thinning and striae (stretch marks) Common uses: inflammatory and pruritic dermatoses (rashes, itching, insect bites) SE: pruritis Burning sensation HPA suppression Monitor: response to treatment – skin atrophy – HPA suppression with long use *Apply sparingly. Wash hands after application Do not cover with bandages/wraps/dressing No improvement in 2 weeks = contact prescriber Overuse = skin thinning and striae (stretch marks) Common uses: inflammatory and pruritic dermatoses – dental paste for oral inflammatory and ulcerative lesions (in mouth) SE: pruritis Burning sensation HPA suppression Monitor: response to treatment – skin atrophy – HPA suppression with long use *Apply sparingly. Wash hands after application Do not cover with bandages/wraps/dressing. Overuse = skin thinning and striae (stretch marks) Dental Paste: apply at bedtime and/or after meal – press small dab onto ulcer – DON’T RUB Topical steroids Notable SE: HPA suppression (Inadequate cortisol production) = When enough Cortisol is not produced, response to stress/defense against infections is impaired => this can lead to adrenal crisis (medical emergency due to lack of cortisol) - Symptoms of HPA suppression: dizzy, weakness, sweating, abdominal pain, nausea, vomiting, loss of consciousness, death due to electrolyte imbalance leading to cerebral/pulm edema. Ocular changes: steroid induced glaucoma – cataract forms – delayed wound healing – more susceptible to infection Signs of bacterial/fungal infection Inhaled Steroids: MOA = inhibits inflammatory cells [mast cells, eosinophils, basophils, lymphocytes, macrophages, neutrophils] + release inflammatory mediators (histamine, eicosanoids, leukotriene, and cytokines) Beclomethasone (Qvar Redihaler) Common Uses: Treat asthma SE: allergic rhinitis, sinusitis, oropharyngeal pain, URTI, nasopharyngitis Monitor: response to treatment, sign/symptoms of oral candidiasis, HPA suppression, glaucoma/cataracts Inhaler: Don’t prime or shake before use Don’t open cap until ready to use – If more than 1 dose, recap before next inhalation Don’t use with spacer. Rinse mouth and spit to prevent thrush Nasal, Inhaled, and Topical steroids: MOA = inhibits inflammatory cells [mast cells, eosinophils, basophils, lymphocytes, macrophages, neutrophils] + release inflammatory mediators (histamine, eicosanoids, leukotriene, and cytokines) Mometasone (Nasonex, Asmanex, Elocon): Common uses: allergic rhinitis, nasal polyps, asthma, dermatoses SE (nasal): epistaxis (nosebleeds), cough, headache SE (inhaler): nasopharyngitis, headache, sinusitis, influenza SE (topical): skin atrophy, burning, pruritis. Monitor: response to therapy, HPA suppression, glaucoma/cataract, nasal effect (perforation, ulceration, irritation, epistaxis, infection) Nasal: pt needs several days before rhinitis symptoms improve (1-2 wks for max benefit) Inhaler: rinse mouth with water and spit out => prevent oral thrush Topical: don’t cover with bandage/wrap/dressing + don’t use on face, groin, axillae Ocular Steroids: MOA = phospholipase A2 inhibitory proteins stimulated => release of arachidonic acid blocked which means leukotrienes and prostaglandin (inflammatory response) are not produced Loteprednol (Lotemax, Alrex, Inveltys) Common use: Ophthalmic inflammation (even post-operative), seasonal allergic conjunctivitis SE: ocular pain/discomfort, blurred vision, foreign body sensation (there’s something in your eye) Monitor: intraocular pressure if med used for 10+ days – look for sign/symptoms of infection Prolonged use => leads to glaucoma with damage to optic nerve/ defect in vision Lotemax: don’t wear contact lenses during therapy. Alrex: remove contact lens before instilling medication (Wait 10 mins before lens is reinserted) Inveltys: remove contact lens before instilling medication (Wait 15 mins before lens is reinserted) Oral Steroids: Dexamethasone (Decadron) Methylprednisone (Medrol) Prednisolone (Orapred, Millipred) Prednisone (Deltasone, Rayos) MOA: inhibiting inflammatory cells and release of inflammatory mediators = suppress inflammation Common use: inflammatory & allergic disease – endocrine disorders – respiratory – rheumatic disorders SE (short-term): insomnia, stomach upset, fluid retention, increased appetite. SE (long-term): Cushing’s syndrome, osteoporosis, muscle wasting, growth suppression in children Monitor: response to therapy, BP, potassium, swelling, blood glucose, intraocular pressure {Used more than 6 weeks = HPA suppression, weight gain} *Take w/ food to decrease GI upset Taper dose to prevent withdrawal symptoms (if used more than 2 wks) Long-term steroid use = don’t give live/live attenuated vaccine (med induced immunosuppression) Don’t use in pt with systemic fungal infections. MOA: bind to cytoplasmic receptors – enters the nucleas – transcription => protein and enzymes involved with inflammation are synthesized Common use: inflammatory & allergic disease – endocrine disorders – respiratory – rheumatic disorders SE (short-term): insomnia, stomach upset, fluid retention, increased appetite. SE (long-term): Cushing’s syndrome, osteoporosis, muscle wasting, growth suppression in children Monitor: response to therapy, BP, potassium, swelling, blood glucose, intraocular pressure {Used more than 6 weeks = HPA suppression, weight gain} *Take w/ food to decrease GI upset Taper dose to prevent withdrawal symptoms (if used more than 2 wks) Long-term steroid use = don’t give live/live attenuated vaccine (med induced immunosuppression) Don’t use in pt with systemic fungal infections. MOA: bind to cytoplasmic receptors – enters the nucleas – transcription => protein and enzymes involved with inflammation are synthesized Common use: inflammatory & allergic disease – endocrine disorders – respiratory – rheumatic disorders SE (short-term): insomnia, stomach upset, fluid retention, increased appetite. SE (long-term): Cushing’s syndrome, osteoporosis, muscle wasting, growth suppression in children Monitor: response to therapy, BP, potassium, swelling, blood glucose, intraocular pressure {Used more than 6 weeks = HPA suppression, weight gain} *Take w/ food to decrease GI upset Taper dose to prevent withdrawal symptoms (if used more than 2 wks) Long-term steroid use = don’t give live/live attenuated vaccine (med induced immunosuppression) Don’t use in pt with systemic fungal infections. MOA: bind to cytoplasmic receptors – enters the nucleas – transcription => protein and enzymes involved with inflammation are synthesized Common use: inflammatory & allergic disease – endocrine disorders – respiratory – rheumatic disorders SE (short-term): insomnia, stomach upset, fluid retention, increased appetite. SE (long-term): Cushing’s syndrome, osteoporosis, muscle wasting, growth suppression in children Monitor: response to therapy, BP, potassium, swelling, blood glucose, intraocular pressure {Used more than 6 weeks = HPA suppression, weight gain} *Take w/ food to decrease GI upset Taper dose to prevent withdrawal symptoms (if used more than 2 wks) Long-term steroid use = don’t give live/live attenuated vaccine (med induced immunosuppression) Don’t use in pt with systemic fungal infections. Cushing syndrome: Body makes too much Cortisol over long period of time.