FINAL PHARM EXAM PDF

+-----------------------------------+-----------------------------------+ | Bronchodilators | | +===================================+===================================+ | Beta-2 Adrenergic Agonists | Activates Beta-2 receptors in the | |...

+-----------------------------------+-----------------------------------+ | Bronchodilators | | +===================================+===================================+ | Beta-2 Adrenergic Agonists | Activates Beta-2 receptors in the | | | lung, causing bronchodilation | | | | | | Selective but systemic effects | | | possible | | | | | | - Tachycardia | | | | | | - Dysrhythmias | | | | | | - Angina | | | | | | - Tremor | | | | | | - Seizures | | | | | | SABAs | | | | | | **Albuterol (ProAir)** | | | | | | **Levalbuterol (Xopenex)** | | | | | | - Inhaled with quick onset of | | | action | | | | | | - PRN to abort acute asthma | | | attack | | | | | | - Goal: use twice a week or | | | less | | | | | | - Available as Metered-Dose | | | Inhaler (MDI), Dry-Powder | | | Inhaler (DPI), or nebulizer | | | | | | - Taking 2 breaths wait one | | | minute between each | | | breath | | | | | | - Administer first | | | | | | - MDI use space to increase | | | medication delivery | | | | | | LABAs | | | | | | **Salmeterol (Serevent Diskus)** | | | | | | **Terbutaline** | | | | | | - Oral or inhaled | | | | | | - Taken on a fixed schedule for | | | long-term control (every 12 | | | hours for inhalers) | | | | | | - Stable COPD LABA preferred | | | | | | - Asthma ALWAYS combine with | | | glucocorticoid | | | | | | - Increased risk of death | | | when used alone for | | | asthma! | | | | | | - FDA recommends combined | | | inhalers | +-----------------------------------+-----------------------------------+ | Methylxanthines | **Theophylline** | | | | | | - Relaxes bronchial smooth | | | muscle | | | | | | - Maintenance of stable asthma | | | | | | - Long duration of action good | | | for nocturnal attacks | | | | | | - Toxicity: | | | | | | - Nausea, vomiting, | | | diarrhea | | | | | | - Restlessness, insomnia | | | | | | - Dysrhythmias | | | | | | - Convulsions | | | | | | - DO NOT CONSUME CAFFEINE | | | increases risk of toxicity | +-----------------------------------+-----------------------------------+ | Anticholinergics | **Ipratropium (Atrovent)\ | | | Tiotropium (Spiriva)** | | | | | | - Blocks muscarinic receptors | | | in bronchi, reducing | | | bronchoconstriction | | | | | | - Only available for inhalation | | | long and short acting forms | | | | | | - May develop anticholinergic | | | effects xerostomia (dry | | | mouth) | +-----------------------------------+-----------------------------------+ | Anti-inflammatory drugs | | +-----------------------------------+-----------------------------------+ | Leukotriene Modifiers | **Montelukast (Singulair)** | | | | | | - Leukotriene receptor blocker | | | blocks activation by | | | leukotrienes | | | | | | - Used to prevent | | | Exercise-induced bronchospasm | | | (EIB) | | | | | | - Associated with | | | neuropsychiatric effects | | | | | | - Take on a regular schedule | +-----------------------------------+-----------------------------------+ | **Cromolyn** | - Reduce inflammation by | | | stabilizing cell membrane of | | | mast cells, reducing | | | histamine and other | | | inflammatory mediators, and | | | by inhibiting eosinophils and | | | other inflammatory cells | | | | | | - Not as effective as | | | glucocorticoids, third-line | | | therapy | | | | | | - Administered via nebulizer | | | | | | - Safest asthma medication | +-----------------------------------+-----------------------------------+ | Medications used for cough, cold, | | | allergy | | +-----------------------------------+-----------------------------------+ | Antihistamines | **Diphenhydramine (Benadryl, | | | Unisom)** | | | | | | **Hydroxyzine (Vistaril)** | | | | | | - Block histamine receptors and | | | some block muscarinic | | | receptors | | | | | | - Lipid soluble with affinity | | | for CNS histamine receptors = | | | crosses BBB | | | | | | - Reduced flushing, edema, | | | itching, mucus production | | | | | | - CNS depression/drowsiness at | | | therapeutic doses | | | | | | - CNS excitation at toxic | | | doses | | | | | | - Anticholinergic effects | | | | | | - Dry mucous membranes | | | | | | - Urinary retention | | | | | | - Constipation | | | | | | - Use in caution with other | | | anticholinergic drugs | | | | | | - Sedation | | | | | | - Do not consume with | | | alcohol | | | | | | - Do not drive or operate | | | heavy machinery | | | | | | Second generation | | | | | | **Fexofenadine (Allegra)** | | | | | | **Loratadine (Claritin)** | | | | | | **Cetirizine (Zyrtec)** | | | | | | - Low-lipid solubility and low | | | affinity for CNS H1 receptors | | | = does not easily cross the | | | BBB | | | | | | - Treats allergy symptoms | | | without CNS or | | | anticholinergic effects | +-----------------------------------+-----------------------------------+ | Sympathomimetics | **Pseudoephedrine (Sudafed)** | | | | | | - Activation of alpha-1 | | | receptors in nose causes | | | vasoconstriction relieving | | | congestion | | | | | | - Rebound congestion when wears | | | off | | | | | | - CNS stimulation (insomnia, | | | irritability, anxiety) | | | | | | - Systemic vasoconstriction = | | | hypertension | | | (contraindication) | | | | | | - Abuse pseudoephedrine can be | | | made into methamphetamine | +-----------------------------------+-----------------------------------+ | Antitussives | **Dextromethorphan** | | | | | | - Suppresses cough reflex in | | | the CNS | | | | | | **Benzonatate (Tessalon)** | | | | | | - Decreases sensitivity of | | | respiratory stretch receptors | | | | | | - Sedation, dizziness, | | | constipation | | | | | | - Capsules must be swallowed | | | whole laryngospasm, | | | bronchospasm, circulatory | | | collapse if chewed | | | | | | - Accidental ingestion by | | | children has been fatal | +-----------------------------------+-----------------------------------+ | Expectorants and Mucolytics | Expectorants | | | | | | **Guaifenesin (Mucinex)** | | | | | | - Increase flow of respiratory | | | secretions to allow for | | | easier expulsion | | | | | | Mucolytics | | | | | | **Hypertonic saline** | | | | | | **Acetylcysteine** (inhaled) | | | | | | - Thins mucus | +-----------------------------------+-----------------------------------+ | Drugs that regulate calcium and | | | bone metabolism | | +-----------------------------------+-----------------------------------+ | **Alendronate (Fosamax)** | - Binds to bone and inhibits | | | osteoclasts | | | | | | - Poorly absorbed and not | | | metabolized | | | | | | - Absorption impaired | | | within 2 hours of Ca | | | | | | - Take with 6-8 oz of water | | | on an empty stomach 30 | | | minutes before other food | | | or drinks | | | | | | - Irritating to stomach and | | | esophagus | | | | | | - Must remain upright for | | | at least 30 minutes | | | | | | - Unbound drug excreted in | | | urine | | | | | | - Reduce dose in | | | mild-moderate renal | | | impairment and | | | discontinue in severe | | | disease | | | | | | - SE-GERD/esophagitis, | | | dysphagia, bloating, | | | flatulence, HA, arthralgias | +-----------------------------------+-----------------------------------+ | **Calcitonin-salmon** | - Inhibits bone reabsorption, | | | increases renal Ca excr5etion | | | | | | - SQ or nasal spray | | | | | | - More effective in | | | hyperparathyroidism, | | | malignancy (hypercalcemia and | | | pain relief) and immobility | | | than in osteoporosis | | | | | | - Well absorbed, but short | | | acting | | | | | | - Alternate nostrils | +-----------------------------------+-----------------------------------+ | **Raloxifene** | - Selective Estrogen Receptor | | | Modulator (SERM) | | | | | | - Estrogen effects on bone | | | | | | - Anti-estrogen effects in | | | breast and uterus | | | | | | - Risk for clots and | | | menopausal symptoms | | | | | | - Metabolized by CYP450 | | | | | | - Excreted mostly in feces and | | | some in urine | +-----------------------------------+-----------------------------------+ | **Teriparatide** | - Recombinant PTH -- 20 mcg SQ | | | QD | | | | | | - Increases osteoblastic | | | activity | | | | | | - Increase Ca absorption | | | and reduces renal Ca | | | excretion | | | | | | - Indicated for severe, | | | unresponsive osteoporosis | | | | | | - Not approved for | | | therapy \> 2 years | | | | | | - Black box warning risk of | | | osteosarcoma | | | | | | - Monitor alk phos, | | | avoid in Paget's | | | | | | - Rapidly and well absorbed | | | | | | - Metabolized by CYP450 and | | | renally excreted | | | | | | - N/V, dizziness, arthralgias, | | | leg cramps | +-----------------------------------+-----------------------------------+ | Drugs for diabetes | | +-----------------------------------+-----------------------------------+ | Short duration rapid acting | **Insulin lispro (Humalog)** | | insulin | | | | - SQ 15 min before or just | | | after meals | | | | | | - SQ cont infusion with bolus | | | just before meals | | | | | | - Approved IV but barely used | | | | | | **Insulin aspart (NovaLog)** | | | | | | - SQ 5-10 minutes before meals | | | | | | - SQ cont infusion with bolus | | | 5-10 min before meals | | | | | | - Approved IV but barely used | | | | | | **Insulin gluilisine (Apidra)** | | | | | | - SQ within 15 min before or | | | within 20 min after meals | | | | | | - SQ cont infusion with bolus | | | 15-20 min before meals | | | | | | - Approved IV but rarely used | +-----------------------------------+-----------------------------------+ | Short duration slower acting | **Regular insulin (Humulin R, | | | Novolin R)** | | | | | | - SQ 30 min before or after | | | meals | | | | | | - SQ infusion cont with bolus | | | 20-30 min before meals | | | | | | - IV for emergencies | | | | | | - IM approved but barely used | +-----------------------------------+-----------------------------------+ | Intermediate duration | **NPH insulin** **(Humulin N, | | | Novolin N)** | | | | | | - SQ twice daily at the same | | | time each day; gently agitate | | | before use | +-----------------------------------+-----------------------------------+ | Long duration | **Insulin glargine (Lantus)** | | | | | | - SQ once daily at the same | | | time each day | | | | | | **Insulin detemir (Levemir)** | | | | | | - SQ twice or once daily | +-----------------------------------+-----------------------------------+ | **Glucagon** | - Hormone produced by alpha | | | cells of the pancreas | | | | | | - Breaks down glycogen stores | | | | | | - Opposite effects of insulin | | | | | | - Used in emergencies if IV | | | glucose cannot be given | | | | | | - If unconscious patient, | | | produces arousal in 20 | | | minutes | | | | | | - Cannot correct hypoglycemia | | | due to starvation | | | | | | - Given IV, SQ, or IM | +-----------------------------------+-----------------------------------+ | Biguanides | **Metformin (Glucophage)** | | | | | | - DOC for initial therapy | | | | | | - Started immediately upon | | | diagnosis | | | | | | - Used alone or in combination | | | | | | - Inhibits glucose production | | | on liver | | | | | | - Slightly reduces glucose | | | absorption in GI tract | | | | | | - Sensitizes insulin receptors | | | in target tissues (increases | | | the cells ability to take in | | | glucose whenever insulin is | | | present) | | | | | | - Does not stimulate release of | | | insulin from the pancreas so | | | it does not drive BG levels | | | down | | | | | | - Absorbed from small intestine | | | | | | - Excreted unchanged by the | | | kidneys | | | | | | - Decreased appetite, nausea, | | | diarrhea, decreased B12 and | | | folic acid deficiency | | | | | | - Toxicity lactic acidosis | | | | | | - Interacts with alcohol and | | | iodinated radiocontrast media | +-----------------------------------+-----------------------------------+ | Sulfonylureas | **Glipizide (Glucotrol)** | | | | | | **Glyburide (DiaBeta, | | | Micronase)** | | | | | | - Stimulate release of insulin | | | from pancreatic islets | | | | | | - Insulin release is glucose | | | dependent | | | | | | - Type II | | | | | | - Can be combined with other | | | hypoglycemic drugs | | | | | | - Hepatic metabolism | | | | | | - Renal excretion | | | | | | - Hypoglycemia | | | | | | - CV toxicity | | | | | | - Interacts with alcohol, beta | | | blockers, other hypoglycemic | | | agents | | | | | | - Contraindicated in pregnancy | +-----------------------------------+-----------------------------------+ | Meglitinides (Glinides) | **Repaglinide (Prandin)** | | | | | | **Nateglinide (Starlix)** | | | | | | - Promotes insulin release | | | | | | - Faster peak and shorter | | | duration of action vs. | | | sulfonylureas | | | | | | - Hepatic metabolism | | | | | | - Biliary excretion | | | | | | - Hypoglycemia | | | | | | - Administered with meals | | | | | | - Gemfibrozil (Lopid) inhibits | | | metabolism | +-----------------------------------+-----------------------------------+ | Thiazolidinediones (Glitazones) | **Pioglitazone (Actos)** | | | | | | - Decrease insulin resistance | | | | | | - Hepatic metabolism | | | | | | - Excretion fecal (main) and | | | urinary | | | | | | - Administer with or without | | | meals | | | | | | - Fluid retention, bladder | | | cancer, unintended pregnancy | +-----------------------------------+-----------------------------------+ | Alpha-glucosidase inhibitors | **Acarbose (Precose)** | | | | | | - Delays absorption of dietary | | | carbohydrates by inhibiting | | | enzyme that breaks down | | | complex carbohydrates to | | | simple carbohydrates | | | | | | - Low absorption; acts locally | | | in the gut, broken down by | | | bacteria/digestive enzymes | | | | | | - Flatulence, cramps, abdominal | | | distention, diarrhea | | | | | | - May cause liver dysfunction | | | | | | - Monitor LFTs every 3 months | | | for first year | | | | | | - Taken at start of meal | | | | | | - Do not cause hypoglycemia | | | alone, but may when used with | | | other agents | | | | | | - In hypoglycemia glucose | | | itself must be used | +-----------------------------------+-----------------------------------+ | Sodium-glucose co-transporter 2 | **Canagliflosin (Invokana)** | | (SGLT-2) Inhibitors | | | | **Dapagliflozin (Farxiga)** | | | | | | - Blocks reabsorption of | | | glucose in the kidney | | | | | | - Increases urinary glucose | | | excretion | | | | | | - Admin before the first meal | | | of the day | | | | | | - Genital yeast infections, | | | UTIs, risk of dehydration, | | | postural hypotension and | | | dizziness | | | | | | - Interacts with diuretics | +-----------------------------------+-----------------------------------+ | DipeptidylPeptidase-4 (DDP-4) | **Sitigliptin (Januvia)** | | Inhibitors (Gliptins) | | | | - Stimulate glucose dependent | | | release of insulin | | | | | | - Suppress post prandial | | | release of glucagon | | | | | | - Rapid and complete absorption | | | with or without food | | | | | | - Peaks in 1-4 hours | | | | | | - Excreted unchanged in the | | | urine | | | | | | - Pancreatitis | | | | | | - Post marketing reports of | | | severe anaphylaxis | +-----------------------------------+-----------------------------------+ | Non-Insulin Injectable | Incretin mimetics | | glucagon-like Peptide (GLP-1) | | | Receptor Agonists | - Incretin is a hormone | | | | | | - Activation causes: | | | | | | - Slow gastric emptying | | | time | | | | | | - Stimulate glucose | | | dependent release of | | | insulin | | | | | | - Inhibit postprandial | | | release of glucagon | | | | | | - Suppress appetite | | | | | | **Dulaglutide (Trulicity)** | | | | | | - Adjunctive therapy to improve | | | glycemic control in patients | | | with type 2 diabetes | | | | | | - Used to improve glucose | | | control in patients taking | | | metformin or sulfonylurea | | | | | | - Given SQ before morning and | | | evening meals | | | | | | - Hypoglycemia with | | | sulfonylurea, GI effects, | | | pancreatitis, renal | | | impairment | +-----------------------------------+-----------------------------------+ | Drugs affecting lipid levels | | +-----------------------------------+-----------------------------------+ | Statins | **Atorvastatin (Lipitor)** | | | | | | - Highly effective and the most | | | prescribed class of | | | antilipemic drugs | | | | | | - Increase HDLs | | | | | | - Decrease LDLs, total | | | cholesterol, VLDLs, and | | | plasma triglycerides | | | | | | - Inhibit HMG-CoA reductase | | | | | | - Promotes formation of LDL | | | receptors in liver | | | | | | - Take at night | | | | | | - Most cholesterol | | | production at night | | | | | | - Contraindicated in pregnancy | | | | | | - Elevated liver enzymes may | | | occur with atorvastatin and | | | all other antilipemic drugs | | | | | | - Monitoring LFTs is essential | | | | | | - Myopathy injury to muscle | | | tissue may occur | | | | | | - Monitor CK at baseline, | | | repeat if symptoms | | | (muscle aches, weakness) | | | occur | | | | | | - Metabolized via the hepatic | | | enzyme CYP3A4 | | | | | | - All drugs and substances | | | that inhibit this pathway | | | may decrease metabolism | | | and increase serum drug | | | concentration | +-----------------------------------+-----------------------------------+ | **Nicotinic Acid Niacin** | - Improves HDL levels by | | | allowing for more circulation | | | of levels in blood | | | | | | - Decreases triglyceride levels | +-----------------------------------+-----------------------------------+ | Bile Acid Sequestrants | **Colesevelam (Welchol)** | | | | | | **Cholestyramine (Questran)** | | | | | | - Binds with bile acids in the | | | intestine to make them | | | non-reabsorbable then excrete | | | them | | | | | | - The lowered bile acid | | | level prompts cholesterol | | | to be used to make more | | | bile acid | | | | | | - GI upset | | | | | | - Reduced absorption of many | | | meds, fat soluble vitamins | +-----------------------------------+-----------------------------------+ | Fibric Acid Derivatives | **Gemfibrozil (Lopid)** | | (Fibrates) | | | | - Lowers TG and raises HDL, | | | little effect on LDL | | | | | | - Increases enzymes that | | | break down VLDL while | | | promoting production of | | | HDL | | | | | | - Used to treat high | | | triglycerides | | | | | | - Rash, GI disturbance, liver | | | injury, myopathy, gallstones | +-----------------------------------+-----------------------------------+ | **Ezetimibe (Zetia)** | - Inhibits GI absorption and | | | reabsorption of cholesterol | | | | | | - Myopathy, hepatotoxicity, | | | pancreatitis, cholelithiasis | | | (gallstones) | +-----------------------------------+-----------------------------------+ | Drugs affecting the thyroid | | +-----------------------------------+-----------------------------------+ | **Levothyroxine (Synthroid, | - Synthetic T4 | | Levoxyl)** | | | | - Identical to naturally | | | occurring thyroid hormone | | | | | | - Converted to T3 | | | | | | - Given PO and well absorbed in | | | empty stomach | | | | | | - Administered 30-60 | | | minutes prior to | | | breakfast | | | | | | - IV form available | | | | | | - Highly protein bound | | | | | | - Once per day dosing | | | | | | - Half-life = 1 week | | | | | | - Takes about one month to | | | reach plateau | | | | | | - Thyrotoxicosis (symptoms of | | | hyperthyroidism), | | | osteoporosis, atrial | | | fibrillation | | | | | | - Absorption decreased by: | | | | | | - Calcium supplements | | | | | | - Antacids | | | | | | - Iron | | | | | | - Cholesterol binding | | | agents | | | | | | - Separate dose by 4 | | | hours form drugs that | | | interact | | | | | | - Food | | | | | | - Phenytoin, carbamazepine, | | | rifampin accelerate | | | metabolism of levothyroxine | | | | | | - Levothyroxine increases | | | effects of warfarin | | | | | | - Thyroid hormones increase the | | | responsiveness to | | | catecholamines... use | | | cautiously | | | | | | - Levothyroxine can increase | | | the requirements of insulin | | | and digoxin | | | | | | - Need to increase dose during | | | pregnancy | | | | | | - Pediatric use: | | | | | | - Continue through age 3 | | | | | | - Stop for 4 weeks to | | | see if hypothyroidism | | | is transient or | | | permanent | | | | | | - Monitor height and | | | development in infants and | | | children | | | | | | - Teach to take on empty | | | stomach | | | | | | - Frequent follow up and lab | | | monitoring TSH preferred | | | method to check for euthyroid | | | | | | - Different brands of | | | levothyroxine may not work | | | the same | | | | | | - Blood work after 6 weeks | | | if changing formulation | +-----------------------------------+-----------------------------------+ | **Methimazole (Tapazole)** | - First line drug | | | | | | - Inhibits thyroid hormone | | | synthesis | | | | | | - Does not destroy existing | | | stores of thyroid hormone | | | | | | - Can take 3-12 weeks to | | | achieve a euthyroid state | | | | | | - Safer than PTU (first | | | trimester) | | | | | | - PO | | | | | | - Applications: | | | | | | - Graves' disease | | | | | | - Adjunct to radiation | | | therapy | | | | | | - Suppress thyroid | | | synthesis in preparation | | | for thyroidectomy | | | | | | - Avoid in 1^st^ trimester of | | | pregnancy | | | | | | - May induce hypothyroidism | | | reduce dose | | | | | | - Agranulocytosis most serious | | | and dangerous toxicity | | | | | | - Report sore throat, fever | | | immediately | +-----------------------------------+-----------------------------------+ | **Propylthiouracil (PTU)** | - Second line drug generally | | | not preferred over | | | methimazole | | | | | | - Risk of liver injury | | | | | | - Shorter half-life | | | requiring multiple | | | doses/day | | | | | | - Can also cause | | | agranulocytosis | | | | | | - Suppresses synthesis of | | | thyroid hormones and | | | conversion of T4-T3 in the | | | periphery | | | | | | - Preferred during thyroid | | | storm/thyrotoxic crisis | | | | | | - Does not cross placenta as | | | easily as methimazole | | | | | | - Preferred during 1^st^ | | | trimester of pregnancy | +-----------------------------------+-----------------------------------+