Final Study Guide - Pharm PDF

# Final Study Guide - Pharm ## Corticosteroids - Hormones produced by the adrenal cortex - Affect almost all body organs - Extremely important in maintaining homeostasis when secreted in normal amounts - Inadequate or excessive secretion leads to disease ### Exogenous Corticosteroids - **Predniso...

# Final Study Guide - Pharm ## Corticosteroids - Hormones produced by the adrenal cortex - Affect almost all body organs - Extremely important in maintaining homeostasis when secreted in normal amounts - Inadequate or excessive secretion leads to disease ### Exogenous Corticosteroids - **Prednisone** - prototype - **Other drugs** - Beclomethasone - Betamethasone - Budesonide - Cortisone - Dexamethasone - Flunisolide - Fluticasone - Hydrocortisone - Methylprednisolone - Prednisolone - Triamcinolone ### Action - Bind drug receptors on target cells, increasing or decreasing protein synthesis - **Resulting in decreased inflammatory response:** - Decreased edema by reducing chemicals that cause vasodilation and tissue irritation. - Immunosuppression: inhibits phagocytosis, impairs lymphocytes, and inhibits tissue repair. ### Uses: To control symptoms (do not cure disease processes) - Allergic or hypersensitivity disorders - Collagen disorders (Lupus) - Dermatologic disorders (dermatitis) - Endocrine disorders (adrenocortical insufficiency) - GI disorders (ulcerative colitis & Crohn's) - Hematologic disorders (idiopathic thrombocytopenic purpura) - Hepatic disorders with edema - Neoplastic disease (leukemia, Hodgkin’s lymphoma) - Corticosteroids inhibit cell reproduction, cytotoxic to lymphocytes - Control symptoms of: - Nausea and vomiting - Cerebral edema - Inflammation from metastasis - Neurologic conditions (cerebral edema, spinal cord injury) - Ophthalmic disorders (optic neuritis) ## Uses Continued - Organ or tissue transplants - Renal disorders with edema - Respiratory disorders (asthma, COPD, rhinitis) - Allergic rhinitis: nasal spray to decrease mucus secretion and inflammation. Systemic effects are minimal. - Asthma: - Increase the effects of adrenergic bronchodilators, given orally or intravenously for 5-10 days. - Tapered after acute symptoms subside. - Inhaled corticosteroids are started during the taper. - **Black Box Warning:** Transferring from systemic to inhaled flunisolide has caused adrenal insufficiency and death. - Rheumatic disorders (ankylosing spondylitis, bursitis, arthritis) - Relieve pain, edema, and mobility restrictions from joint inflammation. Given short-term basis oral or joint injection - Shock from Addisonian crisis ## Adverse Effects: - Adrenocortical insufficiency - Cushingoid features (moon face) - Vertigo - Insomnia - CV effects - Decreased immunity ## Contraindications: - Used cautiously in: - Renal & hepatic impairment - Elderly - Patients with fungal infections - No live virus vaccinations if on steroids - Licorice potentiates the effects of corticosteroids ## Administration: - Localized whenever possible - **Can be delivered in:** - Divided doses - Daily - Every other day (alternate-day therapy) - Stress dosing: chronic corticosteroid users get an increased dosage during stress/illness # Drug Therapy for Disorders of the Eye ## Drugs for Glaucoma #1 ### Prostaglandin analogs: - Most widely prescribed glaucoma drugs. - **Prototype:** Bimatoprost (Latisse, Lumigan) - For open-angle glaucoma, ocular hypertension. - **Action:** Ocular hypotension. - **Use:** Open-angle glaucoma and ocular hypertension. - **Adverse effects:** Hyperpigmentation. ### Beta-adrenergic blockers: - **Prototype:** Timolol maleate - For chronic open-angle glaucoma, aphakic glaucoma, secondary glaucoma, and ocular hypertension. - **Action:** Blocks beta1 and beta2 to reduce intraocular pressure. - **Use:** Chronic open-angle glaucoma and ocular hypertension. - **Adverse effect:** Pain, systemic beta-adrenergic effects. ### Alpha2-adrenergic agonists: - **Prototype:** Brimonidine - For open-angle glaucoma, ocular hypertension. - **Action:** Reduces aqueous humor production. - **Use:** Lowers intraocular pressure. - **Adverse effects:** - CV effect: hypo or hypertension, brady or tachycardia. - **Contraindications:** 14-day washout for MAOI. ### Cholinergic drugs: - **Prototype:** Pilocarpine - For chronic simple glaucoma, chronic and acute angle-closure glaucoma. - **Action:** Stimulates cholinergic receptors in the eye, loss of accommodation and lowers intraocular. - **Use:** Chronic simple glaucoma. - **Adverse effects:** - Burning, conjunctival vascular congestion, CNS: headache, cardiopulmonary: hypertension, tachycardia, bronchial spasm, GI: nausea and vomiting, diarrhea, and increased salivation. ### Carbonic anhydrase inhibitors: - **Prototype:** Acetazolamide (oral), brinzolamide, dorzolamide - For open-angle and secondary glaucoma. - **Action:** Inhibits carbonic anhydrase in the eye reducing the rate of aqueous humor formation and lowering intraocular pressure. - **Use:** Open-angle glaucoma. - **Adverse effects:** Stevens-Johnson syndrome, agranulocytosis, anemia, metabolic acidosis. ### Osmotic drugs: - **Prototype:** Mannitol - Temporarily reduces IOP in acute attacks of glaucoma, also used for reduction of IOP prior to surgery. ### Antibacterial drugs: - For corneal ulcer and bacterial conjunctivitis. - **Prototype:** Fluoroquinolone: ciprofloxacin - Most commonly prescribed. ### Antiviral drugs: - For primary keratoconjunctivitis, recurrent epithelial keratitis. - **Prototype:** Trifluridine - Most commonly administered. ### Antifungal drugs: - For fungal blepharitis, conjunctivitis, and keratitis - **Prototype:** Natamycin ### Antiallergic drugs: - For vernal keratitis, vernal conjunctivitis, and vernal keratoconjunctivitis - **Prototype:** Cromolyn sodium - Decreases or stops the body’s reaction to an allergen. ### H1-receptor antagonists: - Ocular pruritus - **Prototype:** Emedastine difumarate - **Adverse effects:** 11% report headache. ### Corticosteroids: - **Prototype:** Dexamethasone - Decreases inflammation. ### Anti-inflammatory drugs: - Reduces inflammation after cataract extraction, used with corneal refractive surgery. - **Prototype:** Diclofenac ### Immunosuppressants: - Increases tear production. - **Prototype:** Cyclosporine emulsion ## General Guidelines for Ophthalmic Drug Therapy: - Topical administration is the most common route. - Correct administration is essential for optimal therapeutic effects. - Systemic absorption can be decreased by occluding the lacrimal duct. - Multiple drop types need 5- to 10-minute intervals between administrations. - Absorption decreased with eye inflammation. - Systemic absorption of ophthalmic drugs can be decreased by occlusion of the lacrimal duct for 3 to 5 minutes after instillation. # Drug Therapy for Disorders of the Ear ### Otitis Externa - Disorder of the external ear that produces inflammation, also known as swimmer’s ear. - Caused by: - Moisture in the ear canal - Allergic reactions such as psoriasis - Trauma of the ear canal related to itching or scratching. - **Use of topical agents is most common, effective way to deliver high concentrations of medication to infected tissue.** - **Systemic medications are used if deep tissue infection develops outside the external canal or if the patient is immunocompromised.** - **When infection extends to the pinna, oral anti-infective agents are used.** ### Otitis Media - More common in children than in adults, pathogens enter the middle ear as a result of an alteration in the eustachian tube. - Can be caused by: - Upper respiratory congestion - Inflammation - Allergic reaction - Bacteria may enter the middle ear from contaminated secretions of the nasopharynx or perforation of the tympanic membrane. - **Oral amoxicillin is the drug of choice.** - **Those allergic to penicillins may take cephalosporins.** ## Anti-infective, antiseptic, glucocorticoid, and acidifying agents. - **Prototype:** Neomycin-polymyxin B-hydrocortisone - combination drug, antibiotics and steroid. - For acute external otitis media (topical agent, -otic drops). - **Action:** Each drug in the combo has its own mechanism of action to inhibit bacterial growth or limit the inflammatory process. - **Use:** Acute otitis externa. - **Adverse effects:** Sensitivity. ### Fluoroquinolone - **Prototype:** Ciprofloxacin - Drug of choice for necrotizing otitis externa (IV then oral). - **Action:** Inhibits bacterial growth. - **Use:** Treatment of necrotizing otitis externa. - **Adverse effects:** As per antibiotic lecture ### Antibacterial agent - **Prototype:** Amoxicillin (a penicillin) - **Action:** Inhibits cell wall synthesis of sensitive organisms, resulting in cell death. - **Use:** For acute otitis media. - **Adverse effects:** Include hypersensitivity to drugs, GI effects, and development of superinfections. ## Patient Guidelines: - Take the entire course of anti-infective agents. - Take adjuvant medications to reduce pain and fever. - Do not insert items in the ear. - Use earplugs when swimming. - Dry ear carefully following bathing or swimming. # Drug Therapy for Disorders of the Skin ## Guidelines for Dermatologic Drug Therapy: - Drug selection dependent on: - Condition or factors, including acuity, severity, location, extent. - Drug dose dependent on drug strength, area, and method of application. - Agent choice dependent on reason for use, patient response. ## Types of Dermatologic Drugs: ### Antimicrobials - topical presentation #### Antibacterials - Bacitracin - Benzoyl peroxide - Clindamycin - Erythromycin - Metronidazole - Mupirocin - Silver sulfadiazine - Nystatin #### Antifungals - Butenafine - Ciclopirox - Clotrimazole - Ketoconazole - Nystatin #### Antivirals - Acyclovir - **Use:** To treat bacterial, fungal and viral infections of the skin. - **Application can be oral, topical, or parental.** ### Antiseptics: - **Action:** Kill or inhibit growth of bacteria, viruses, or fungi. - **Uses:** Primarily used to PREVENT infection. ### Corticosteroids: - **Uses:** Topical for dermatitis to decrease inflammation. ### Emollients and moisturizers: - **Uses:** Lubricants. ### Enzymes: - **Trypsin** - **Uses:** Debride wounds. ### Immunosuppressants: - **Pimecrolimus, Tacrolimus - both topical** - **Uses:** Treat inflammatory skin conditions (psoriasis). ### Keratolytics: - **Uses:** Keratin-containing skin conditions. ### Retinoids (Isotretinoin): - **Action:** Suppression of sebum production. - **Uses:** Primarily acne. - **Adverse effects:** Strictly regulated by FDA because of severe reproductive, and psychiatric effects, commonly causes dryness, arthralgia, hyperlipidemia. - **Contraindications:** Black Box warning - pregnancy category X. ### Sunscreens # Drug Therapy for Hyperthyroidism and Hypothyroidism ## Hyperthyroidism - Excessive secretions of thyroid hormone - from problems with the thyroid or too much TSH. - **Graves’ disease, goiter** ## Hypothyroidism - Inadequate production of thyroid hormones. - **Primary:** Thyroiditis - **Secondary:** Decreased TSH and TRH ## Hypothyroidism - **Cardiovascular:** - Decreased cardiac output - Decreased blood pressure & heart rate - Enlarged heart - **CNS:** - Lethargy - Slow speech, slurring - Forgetfulness, mental sluggishness - Excessive drowsiness - **Metabolic:** - Cold intolerance - Subnormal temp - Weight gain - **Gastrointestinal:** - Decreased appetite - Constipation - **Integumentary:** - Dry, coarse, thick skin - Puffey face & eyelids - **Reproductive:** - Dry & thin hair, thick hard nails - Prolonged menstrual periods, infertility, decreased libido - **Miscellaneous:** - Increased susceptibility to infection ## Hyperthyroidism - **Cardiovascular:** - Increased cardiac output - Increased systolic blood pressure and tachycardia - Dysrhythmias - **Nervousness:** - Nervousness - Restlessness - Anxiety - Insomnia - **Metabolic:** - Heat intolerance - Low-grade fever - Weight loss - Increased appetite - **Gastrointestinal:** - Diarrhea, nausea & vomiting - **Integumentary:** - Moist, flushed skin (vasodilation & increased sweating) - Localized eye edema - **Reproductive:** - Eye changes, exophthalmos - Hair & nails soft - Amenorrhea - **Miscellaneous:** - Increased susceptibility to infection ## Drugs used for Hyperthyroid disease: - **Prototype:** Propylthiouracil - Used to treat hyperthyroidism, also, Methimazole - **Mechanism of action:** Decreasing production or release of thyroid hormones - **Indications for use:** Hyperthyroidism secondary to: Graves’ disease, nodular goiter, Thyroiditis, functioning thyroid carcinoma, Pituitary adenoma, thyroid storm - **Adverse effects:** Hypothyroidism, GI upset - **Interactions:** Anticoagulants (increased risk for bleeding) - **How do we assess effectiveness?** - **Adjuvant medication:** Propranolol - Beta-adrenergic blocker controlling symptoms of hyperthyroidism ## Drugs used for Hypothyroid disease: - **Prototype:** Levothyroxine - **Mechanism of action:** Provide exogenous source of thyroid hormones, best absorbed on an empty stomach - **Black Box Warning:** Thyroid hormones for the treatment of weight loss - **Adverse effects:** s/s of hyperthyroidism - **Interactions:** Some antidepressants and beta-adrenergic agents, nasal decongestants increase the effects of thyroid hormones; antacids, cholestyramine, iron, sucralfate decrease absorption # Drug Therapy for Pituitary and Hypothalamic Dysfunction ## Posterior Pituitary Hormones - Posterior pituitary gland stores and releases two hormones that are synthesized by nerve cells in the hypothalamus. - **Antidiuretic hormone (ADH)**, also called vasopressin - causes water to be resorbed into the tubules - **Oxytocin** - will be addressed in Women’s Health Lecture ## Diabetes Insipidus: - Results from dysfunction of the posterior pituitary. - Absence of Antidiuretic hormone cause the kidneys to filter water and not reabsorb it. - Large urine production (4 to 30 liters), decreased circulating volume, increased thirst. - **Prototype drug is desmopressin acetate, synthetic of ADH:** - **Mechanism of action:** Reduces urine volume and serum osmolality, increases reabsorption of water by the kidney. - **Use:** Treatment of Diabetes Insipidus. - **Black Box Warning:** Severe hyponatremia, changes in fluid volume can result in cardiac arrest. # Drug Therapy to Regulate Calcium and Bone Metabolism ## Calcium and Bone Metabolism - **Three hormones:** - Parathyroid hormone (PTH) - Calcitonin - Vitamin D - **Hypocalcemia, hypercalcemia - both can be life threatening** ### Hypocalcemia - **Characterized by:** Increased resorption of calcium & Loss of bone mass. - **Weaken bones:** Lead to fractures, pain, disability. - **Principles of Drug Therapy:** Restore normal calcium balance in body and prevent: - Osteoporosis treatment - Bisphosphonates, calcitonin, estrogens, and antiestrogens. - **Calcium carbonate or calcium citrate - oral:** Oral calcium can interfere with absorption of other oral medications. - **IV calcium is essential for the treatment of acute, severe hypocalcemia (medical emergency).** ### Vitamin D: - **Action:** Increases Ca and Phosphorus absorption in the Gl tract. - **Adverse effect:** Hypercalcemia. ### Bisphosphonates: - Inhibit calcium resorption from bone. - **Prototype:** Alendronate (Fosamax) - **Action:** Binds to bone and reduces breakdown. - **Use:** Treat osteoporosis in post-menopausal women and osteoporosis in men. - **Adverse effect:** Limited if taken as ordered: - Take upon waking with 6-8 oz of water, at least 30 min before eating or drinking anything else. - Must sit upright or stand for at least 30 minutes following administration. ### Hypercalcemia: - **Calcitonin:** Treatment of hypercalcemia, Paget's disease, and postmenopausal osteoporosis. - **Acute hypercalcemia (severe symptoms or a serum calcium level greater than 14 mg/dL):** A medical emergency & Rehydration is a priority. - Administer an IV saline solution (0.9% sodium chloride) at an initial rate of 200 to 300 mL/h and then adjust it to maintain a urine output of 100 to 150 mL/h. # Drug Therapy for Myasthenia Gravis, Alzheimer's Disease, and Other Conditions Treated with Cholinergic Agents ## Myasthenia gravis: - Neuromuscular conditions characterized by disruptions in neurologic and autoimmune processes. - **Acetylcholinesterase inhibitor drugs:** - **Prototype:** Neostigmine - IV use only, also used as an antidote for tuborcurarine and skeletal muscle relaxants given during surgery, more commonly prescribed: pyridostigmine. - **Use:** Diagnosis and treatment of Myasthenia gravis. - **Action:** Acetylcholine builds up in the synapse, decreased heart rate, increase smooth muscle tone, increased salivary secretions. - **Adverse Effects:** Cardiovascular effects, increased secretions. - **Contraindications:** Renal and hepatic impairment, asthma, CV disease. ## Alzheimer's Disease: - Most common form of dementia, deficiency in cholinergic function in the cortex and basal forebrain, neuropathologic hallmarks are neuritic plaques and neurofibrillary tangles. - **Early symptom:** Difficulty remembering newly learned information. - **Advanced symptoms:** - Disorientation and mood and behavior changes, deepening confusion about events, time, and place. - Unfounded suspicions about family, friends, and professional caregivers. - More serious memory loss and behavior changes, and difficulty speaking, swallowing, and walking. - **Goal of therapy:** Slow memory and cognition loss, preserve individual’s independence for as long as possible. ### Cholinesterase inhibitors: - Reversible indirect-acting cholinergics. - **Prototype:** Donepezil (Aricept), rivastigmine (Exelon) - **Action:** Increases acetylcholine in the brain, slowing neuronal degradation. - **Uses:** Delay progression of Alzheimers disease up to 55 weeks, enhances memory in MS. - **Adverse effects:** Headache, dizziness, depression, vertigo, Gl disturbances, dyspnea in patients with past lung disease. - **Contraindications:** Lung disease, or heart disease. ### N-methyl-d-aspartate receptor antagonist: -**Prototype:** Memantine (Namenda) - **Action:** Antagonizes the NMDA receptor. - **Uses:** Slow progression of moderate to severe Alzheimer’s disease. - **Contraindications:** Renal failure. ## Urinary Retention - **Causes:** - Most common is a lack of nerve innervation (neurogenic bladder). - Others include diabetes, prostate enlargement, pregnancy, neurologic disorders such as multiple sclerosis or Parkinson’s disease, and surgery with general anesthesia. ### Cholinergic agonist: - **Prototype:** Bethanechol chloride (Urecholine) - **Action:** Acts like acetylcholine, increase urinary and Gl muscle tone. - **Use:** Acute postop for treatment of nonobstructive urinary retention, and neurogenic atony of the bladder. - **Adverse effects:** Heart block, orthostatic hypotension, Gl adverse effects, urinary urgency. - **Contraindications:** Bladder neck surgery. # Drug Therapy for Parkinson's Disease, Urinary Spasticity, and Disorders Requiring Anticholinergic Drug Therapy ## Parkinson's Disease: - A chronic, progressive, degenerative disorder of the CNS characterized by resting tremor, bradykinesia, rigidity, postural instability, Shuffling gait, stooped posture, masklike facial expression, soft-speaking voice. - **Initial:** Resting tremor that begins in fingers and thumb of one hand, pill-rolling movements. ### Dopamine Receptor Agonists: - Increase the amount of dopamine in the brain via various mechanisms: - **Prototype:** Levodopa-carbidopa (Sinemet), Amantidine, pramipexole, ropinirole. - **Action:** Increase dopamine in the synapse. - **Uses:** Parkinson’s, Restless Leg Syndrome. - **Adverse effect:** Headache, anxiety, hallucinations, drowsiness, CV effects. - **Contraindications:** Glaucoma, severe hypertension, MAO inhibitors, severe cardiovascular, pulmonary, renal, hepatic, or endocrine disorders. ### Catechol-O-Methyltransferase Inhibitors: - **Prototype:** Tolcapone - Increases dopamine levels in the brain. - **Action:** Inhibits levodopa metabolism. - **Use:** Treat s/s of idiopathic Parkinson’s, Use only in conjunction with levodopa-carbidopa. Relieves symptoms effectively and consistently within 3 weeks or treatment is discontinued - **Adverse Effects:** CNS, CV, GI, respiratory system. - **Contraindications** Liver disease, nontraumatic rhabdo. ### Anticholinergics: - Atropine, benztropine mesylate, glycopyrrolate, ipratropium bromide, dicyclomine hydrochloride, oxybutynin chloride, scopolamine hydrobromide. - **Action:** Antispasmodic and antisecretory action. Effects in CNS, heart, smooth muscle, glands, eye. - **Use:** Idiopathic parkinsonism with minimal symptoms, patients intolerant of levodopa, used in combination therapy, relieve symptoms of extrapyramidal reaction, not effective for bradykinesia, decrease salivation, spasticity, and tremors. - **Contraindications:** Glaucoma, myasthenia gravis, Gl obstruction, prostatic hypertrophy, Urinary bladder neck obstruction, Cardiovascular disorders, Hepatic or renal disease, Elderly patients with cognitive impairments. ### Belladonna alkaloid: - **Atropine:** - **Action:** Depresses salivary and bronchial secretions. - **Use:** Cardiac rate restoration. - **Adverse effects:** Anticholinergic effects. ### Centrally acting anticholinergics: - **Benztropine mesylate (Cogentin):** - **Action:** Suppresses secondary symptoms of parkinsonism. - **Use:** Parkinsonian symptoms. - **Adverse effects:** Anticholinergic effects. - **Contraindications:** Glaucoma, GI & GU obstruction, CV disorders. ### Gastrointestinal anticholinergics: - Dicyclomine hydrochloride (Bentyl): - **Action:** GI smooth muscle relaxant. - **Use:** Treat irritable bowel syndromes - **Adverse effects:** Anticholinergic effects - **Contraindications:** Glaucoma, asthma, GI & GU obstruction ### Urinary antispasmodics: - Oxybutynin (Ditropan): - **Action:** Relaxes smooth muscle. - **Use:** Bladder instability, overactive bladder, incontinence, urgency, frequency. - **Adverse effects:** Anticholinergic effects. - **Contraindications:** Ulcers, obstructions.