Drug Classifications Drugs are a diverse and fall into many categories The most common categories of medications will be covered here There are others but in the interest of importance and simplicity the following lecture should provide a general starting point

Analgesics Narcotics MOA: bind to opiate receptors in brain and spinal cord Indications: Analgesia Main Side effects: N/V, constipation, physical and psychological dependence. In overdose , respiratory depression. See text for complete list. Fentanyl is available as a IV injection, patches, oral lozenges but not as a tablet Oxycodone is not available as an injection only orally High potency opiates include fentanyl, remifentanil and hydromorphone (Dilaudid®) . High risk of overdose Combination product: Tylenol with Codeine denoted as follows Tylenol#2 as Codeine 15 mg/APAP 300 mg Tylenol #3 as Codeine 30 mg/APAP 300 mg Tylenol#4 as Codeine 60 mg/APAP 300 mg

Anti-Infectives Indications: Agents that are used to treat microrganism infection in the body MOA: various (see next slide) The class include: Antibiotics : Penicillins and cephalosporins Antivirals: Acyclovir, ganciclovir, Antituberculosis-isoniazid, ethambutol, pyrazinamide Antiretrovals: NRTI: Zidovudine, NNRTI-efavirenz, PI-ritonavir Fluoroquinolones: ciprofloxacin, levofloxacin Antimalarial: (treat miliaria): quinine sulfate Antifungals: Fluconazole (Diflucan®), amphotericin (Amphocin®) Please see table 20-2 in the textbook for a complete list

Antibiotic mechanism of action Penicillin and Cephalosporins: drugs inhibit the formation of the bacterial cell wall. Bacteria swell and die. Drugs are bactericidal Macrolides: inhibits bacterial ribosomes and protein synthesis. Example includes erythromycin (E-Mycin®) and azithromycin (Zithromax®). Bactericidal or Bacteriostatic. Tetracyclines: Bacteriostatic by inhibiting protein synthesis. Fluroquinolones: Bactericidal. Binds to DNA gyrase Aminoglycosides: (Gentamicin) Bactericidal by several mechanisms

Very important antibiotics Penicillins and Cephalosporins are classified as Beta Lactam antibiotics. Very important antibiotics Treats a wide variety of bacterial infections Penicillins are several classes Class Example Brand name Natural Penicillin Penicillin G Pfizerpen (IV form) Aminopenicillin Ampicillin Omnipen Ureidopenicillin Piperacillin/Tazobactam Zosyn Penicillinase resistance penicillins Nafcillin Nafcil

Main Side Effects of penicllins/cephalosporins Nausea/Vomiting Diarrhea Type I hypersensivity Cephalosporins Chemically similar to penicillins (Beta lactam) Four generations Excellent antibiotics Similar side effects

Generation Generic Brand First Cephalexin Keflex (oral only) Cefazolin Ancef (IV) Second Cefaclor Ceclor (oral only) Cefuroxime Ceftin (oral suspension) Zinacef (IV) Third Ceftriaxone Rocephin (IV only) Cefdinir Omnicef (oral only) Fourth Cefipime Maxipime Carbapenems Meropenem Merrem Third and fourth generations are used to treat meningitis and hospital acquired infections and pneumonias

Fluoroquinolones Must take oral forms of these drugs separate from antacids (Maalox) by 1-2 hours Many drug interactions Advised to limit the consumption of caffeine while on these drugs (ciprofloxacin more than others) Generic Brand Ciprofloxacin Cipro Levofloxacin Levaquin Moxifloxacin Avelox Lomefloxacin Maxaquin

Tetracyclines Broad spectrum antibiotic class Effective for use in certain infections Clamydial infections: doxycycline Lyme Disease: Doxycycline or Minocycline Don’t use tetracycline in pregnant women Avoid use in young children CAUTION: never use expired tetracycline products. Toxin produces serious kidney damage CAUTION: advise patient to wear protective clothing. Drugs are photosensitive chemicals

Non Steroidal Anti Inflammatory Drugs Called the NSAIDS Excellent drugs for pain relief and reducing fever and inflammation Developed as an alternative to corticosteroids MOA: blocks the COX enzyme to block prostaglandin formation Side effects are: severe GI bleeding (possible), GI upset and gastritis, kidney insufficiency, edema and elevated blood pressure, hyperkalemia risk Generic Brand Ibuprofen Motrin, Advil Naproxen Naprosyn Ketorolac Toradol (IV available) Diclofenac Voltaren Celecoxib Celebrex (COX2 inhibitor)

Cardiovascular Drugs Beta Blockers: drugs that block the beta receptors in the heart which blocks attachment of norepinephrine and results in bradycardia and reduced blood pressure. Examples are propranolol(Inderal®), metoprolol (Toprol XL, lopressor ®), atenolol (tenormin®) This is an important drug used in heart failure patients, patient that have had an MI, and hypertensive patients. ACE inhibitors (angiotensin converting enzyme inhibitor) blocks the enzyme (ACE) responsible to converting angiotensin I to angiotensin II (ATII). ATII is a potent vasoconstrictor in humans. ATII is also important in kidney function. ATII also increases aldosterone secretion. This drug is important in hypertensive patients and patients with CHF and MI. ACEI are also important in preservation of kidney function in diabetics. Examples are enalapril( Vasotec®) and Ramipril (Altace®)

Antianginal agents: used to widen coronary arteries to increase myocardial oxygen delivery and reduce chest pain. Examples: nitroglycerin (NTG), and isosorbide (Imdur®, Isordil®) Calcium channel blockers: blocks the entry of calcium ions in the heart muscle and in the muscle that control blood vessel diameter. Reduced heart rate and reduces blood pressure. Some are used to control a type of cardiac arrhythmia called atrial fibrillation. Examples: Diltiazem (Tiazac®, Cardizem®), amlodipine (Norvasc®) Antiarrhythmial agents: block the entry of sodium into the heart. The drugs in this class have several mechanisms of action. Examples: Lidocaine, amiodarone (Cordarone®), Procainamide (Procanbid®)

Angiotensin 2 Receptor blockers (ARB’s): similar to ACEI except these drug works on a receptor for ATII. Examples are Losartan (Cozaar®), valsartan (Diovan®) Anticoagulation agents: drugs that block the formation of blood clots. Different mechanisms of action. Examples: warfarin (coumadin®), dibigatran (Pradaxa®) Antiplatelet agents: drugs that block the action of platelets in the formation of a blood clot. Used in the prevention of stroke or MI. Examples: Clopidegrel (Plavix®) and Aspirin (Ecotrin®)

Antihyperlipidemics: drugs used to treat high blood lipid levels (cholesterol, triglycerides) Examples are the statin drugs, Niacin (Niaspan®), Omega 3 fatty acid (Lovaza®) Cardiac glycosides: drugs used to boost the strenght of the heart’s contraction. Example: Digoxin (Lanoxin®)

Alpha Receptor blockers MOA: blocks alpha receptors on smooth muscle in the arteries Indication: blood pressure control Side effects: edema, dizziness Examples Prazosin (Minipress) Terazosin (Hytrin) Doxazosin (Cardura) The following alpha blockers are used for enlarged prostate symtom relief Tamsulosin (Flomax) Alfuzoxin (Uroxatral) The following drugs are both alpha and beta receptor blockers Labetolol (Trandate) Carvedilol (Coreg)

Oral Contraceptives Drugs that contain high doses of estradiol and/or progestins MOA: high levels of hormones “tricks” the body to think its pregnant and ovulation don’t occurs Indication: Birth control, vaginal bleeding control, endometriosis Examples: LoOvral Loestrin Yasmin Ortho tri cyclen Federal law mandates that the patient package insert be dispensed with Rx to patient in retail

Diuretics Drugs that work at the kidney to help remove sodium, water, calcium, and potassium from the body. Each class of diuretic is named for the most part according to its mechanism of action or the site of action in the kidney. Loop Diuretics work in a section of the kidney called the loop of henle. This is where most of the water and sodium and potassium is lost from the body. These drugs are used to treat edema in CHF patients and other patient that hold on the water. Example(s): Furosemide (Lasix®), Torsemide (Demadex®)

Carbonic anhydrase inhibitors act on the proximal tubule of the kidney by blocking the enzyme, carbonic anhydrase which cause sodium retention and acid loss. Example: acetazolamide (Diamox®) Carbonic anhydrase inhibitor are pretty much weak diuretics and can produce profound lose of potassium

Thiazide Diuretics Thiazide diuretics act on the distal convoluted tubule to block the NaCL cotransporter in the kidney. Generally good diuretics Produce a sodium rich urine Example: Hydrochlorothiazide (HydroDiuril®)

Potassium Sparing diuretics Most of the above diuretics cause profound lose of potassium. To circumvent this, these diuretic are usually taken with potassium supplements. A class of diuretic that “spares” potassium in the body are know and are used for many indications Examples are: spironolactone (aldactone®), Amiloride (Midamor®), and the ACE inhibitors with ARB’s. These diuretics unlike the ones mentioned before should not be used with a potassium supplement.

Central Nervous System Drugs Sedatives and Tranquiller: Drugs that cause depression of the reticular activating system in the brain. Differences in mechanisms of action. Examples are barbiturates: Phenobarbital (Luminal®) Benziodiazepines: Chlordiazepoxide (Librium®), Diazepam (Valium®), Lorazepam (Ativan®), Alprazolam (Xanax®) BDZ were developed in the 1960’s with the advent of librium®. BDZ are safer than barbiturates. Both dangerous with alcohol consumption. Used in anxiety disorder, panic disorder, GAD, sleep disorders Control Substance: CIV Miscellanous agents in the class are zolpidem (Ambien®), zaleplon (Sonata®)

Neuroleptic agents: drug used in the treatment of schizophrenia and other personality disorders. Examples include: Dopamine block agents: Haloperidol (Haldol®), Chlorpromazine (Thorazine®), Fluphenazine (Prolixin®) Dopamine and serotonin blocking agents: Olanzapine (Zyprexa®) and Quetiapine (Seroquel®)

Drugs used to treat ADHD in children and adults Mixed amphetamine salts: Adderall® XR Other agents: Methylphenidate (Ritalin® Concerta ®, Focalin ®)

Antiepileptics Indications: Drugs used to treat seizures. Off label use: Neuropathic pain MOA: Many of the drugs block the sodium ion channel in nerves. Main Side effects: Drugs in this group are known to cause birth defects Levetiracetam is a known cause of SJS Topiramate can cause kidney stones For emergency tx: use diazepam or phenytoin IV

Generic Brand Phenytoin Dilantin Valproic Acid Divalproex Sodium Depakene Depakote Carbamazepine Tegretol Gabapentin Neurotin Oxcarbazepine Trileptal Levetiracetam Keppra Topiramate Topamax Phenytoin, Valproic acid, Levetiracetam and Diazepam are available as IV injections

Drugs used to treat depression Drugs that block the reuptake of dopamine, serotonin and norepinephrine in the brain are called Tricyclic antidepressants. Drugs in this class include : amitriptyline, nortriptyline. These drugs have fallen into disuse over the decades due to their toxicity in overdose. As little as 1,000 mg of nortriptyline has resulted in fatal overdoses SSRI or selective serotonin reuptake inhibitors are now most commonly used. Examples include: Fluoxetine (Prozac®), Paroxetine (Paxil®) SSRIs have been used for other indications

Drugs used to treat Diabetes Insulin: the nature human hormone needed to clear blood glucose. Examples: Ultrafast: Novolog®, Humalog®, Regular insulin (Humulin®), Basal insulin: Lantus® Sulfonylureas: drugs that increase the release of insulin in the body. Examples include: Glipizide (Glucotrol®), Glyburide. Sulfonylurea should be taken with food Meglitinides: drugs similar to sulfonylurea by faster acting. Examples: Repaglinide (Prandin®, Nateglinide (Starlix®) Thiazolidinediones: drugs that increase the body sensitivity to insulin. Example includes: pioglitazone (actos®) Other agents include: exenatide (Byetta®), sitagliptin (Januvia®) and metformin (Glucophage®)

CNS Depressants Benzodiazepines and Barbiturates MOA: binds to GABA receptors in brain Indications: sedation for anxiety and pre op use Main Side Effect: drowiness, Dependence (CIV) Generic Brand Lorazepam Ativan Clonazepam Klonopin Alprazolam Xanax Midazolam Versed Zolpidem (not a BDZ) Ambien Primidone Mysoline

Skeletal Muscle Relaxants MOA: may block action of calcium in muscles Indications: painful muscle spasms, neurological spinal cord injury Main Side Effects: Drowsiness, weakness Generic Brand Cyclobenzaprine Flexeril Methocarbamol Robaxin Baclofen Lioresal