Книги фарма 2 / Bertram G. Katzung-Basic & Clinical Pharmacology(9th Edition)

Rabeprazole (Aciphex)

Oral: 20 mg delayed-release tablets

Mucosal Protective Agents

Misoprostol (Cytotec)

Oral: 100, 200 g tablets

Sucralfate (generic, Carafate)

Oral: 1 g tablets; 1 g/10 mL suspension

Digestive Enzymes

Pancrelipase (Cotazym, Pancrease, Viokase, others)

Oral: Capsules, tablets, or powder containing lipase, protease, and amylase activity. See manufacturers' literature for details.

Drugs for Motility Disorders & Selected Antiemetics

Alosetron (Lotronex)

Oral: 1 mg tablets

Cisapride (Propulsid)

Available in the USA only from the manufacturer, 877-795-4247

Dolasetron (Anzemet)

Oral: 50, 100 mg tablets

Parenteral: 20 mg/mL for injection

Dronabinol (Marinol)

Oral: 2.5, 5, 10 mg capsules

Granisetron (Kytril)

Oral: 1 mg tablets

Parenteral: 1 mg/mL for injection

Metoclopramide (generic, Reglan, others)

Oral: 5, 10 mg tablets; 5 mg/5 mL syrup, 10 mg/mL concentrated solution

Parenteral: 5 mg/mL for injection

Ondansetron (Zofran)

Oral: 4, 8, 24 mg tablets; 4 mg/5 mL solution

Parenteral: 2 mg/mL for IV injection

Prochlorperazine (Compazine)

Oral: 5, 10, 25 mg tablets; 10, 15, 30 mg capsules; 1 mg/mL solution Rectal: 2.5, 5, 25 mg suppositories

Parenteral: 5 mg/mL for injection

Tegaserod (Zelnorm)

Oral: 2, 6 mg tablets

Selected Anti-Inflammatory Drugs Used in Gastrointestinal Disease

Balsalazide (Colazal)

Oral: 750 mg capsules

Budesonide (Entocort)

Oral: 3 mg capsules

Hydrocortisone (Cortenema, Cortifoam)

Rectal: 100 mg/60 mL unit retention enema; 90 mg/applicatorful intrarectal foam

Mesalamine (5-ASA)

Oral: Asacol: 400 mg delayed-release tablets; Pentasa: 250 mg controlled-release capsules Rectal: Rowasa: 4 g/60 mL suspension; 500 mg suppositories

Methylprednisolone (Medrol Enpack)

Rectal: 40 mg/bottle retention enema

Olsalazine (Dipentum)

Oral: 250 mg capsules

Sulfasalazine (generic, Azulfidine, others)

Oral: 500 mg tablets and enteric-coated tablets

Infliximab (Remicade)

Parenteral: 100 mg powder for injection

Selected Antidiarrheal Drugs

Bismuth subsalicylate* (Pepto-Bismol, others)

Oral: 262 mg caplets, chewable tablets; 130, 262, 524 mg/15 mL suspension

Difenoxin (Motofen)

Oral: 1 mg (with 0.025 mg atropine sulfate) tablets

Diphenoxylate (generic, Lomotil, others)

Oral: 2.5 mg (with 0.025 mg atropine sulfate) tablets and liquid

Kaolin/pectin* (generic, Kaopectate, others)

Oral (typical): 5.85 g kaolin and 260 mg pectin per 30 mL suspension

Loperamide* (generic, Imodium, others)

Oral: 2 mg tablets, capsules; 1 mg/5 mL liquid

Selected Laxative Drugs*

Bisacodyl (generic, Dulcolax, others)

Oral: 5 mg enteric-coated tablets

Rectal: 10 mg suppositories

Cascara sagrada (generic)

Oral: 325 mg tablets; 5 mL per dose fluid extract (approximately 18% alcohol)

Castor oil (generic, others)

Oral: liquid or liquid emulsion

Docusate (generic, Colace, others)

Oral: 50, 100, 250 mg capsules; 100 mg tablets; 20, 50, 60, 150 mg/15 mL syrup

Glycerin liquid (Fleet Babylax)

Rectal liquid: 4 mL per applicator

Glycerin suppository (generic, Sani-Supp)

Lactulose (Chronulac, Cephulac)

Oral: 10 g/15 mL syrup

Magnesium hydroxide [milk of magnesia, Epsom Salt] (generic)

Oral: 400, 800 mg/5 mL aqueous suspension

Methylcellulose

Oral: bulk powder

Mineral oil (generic, others)

Oral: liquid or emulsion

Polycarbophil (Equalactin, Mitrolan, FiberCon, Fiber-Lax) Oral: 500, 625 mg tablets; 500 mg chewable tablets

Polyethylene glycol electrolyte solution (CoLyte, GoLYTELY, others) Oral: Powder for oral solution, makes one gallon (approximately 4 L)

Psyllium (generic, Serutan, Metamucil, others)

Oral: 3.3, 3.4, 3.5, 4.03, 6 g psyllium granules or powder per packet

Senna (Senokot, ExLax, others)

Oral: 8.6, 15, 17, 25 mg tablets; 8.8, 15 mg/mL liquid

Drugs That Dissolve Gallstones

Monoctanoin (Moctanin)

Parenteral: 120 mL bottle for bile duct perfusion

Ursodiol (Actigall)

Oral: 300 mg (Actigall) capsules *Over-the-counter formulations.

Chapter 64. Therapeutic & Toxic Potential of Over-the-Counter

Agents

Katzung PHARMACOLOGY, 9e > Section X. Special Topics > Chapter 64. Therapeutic & Toxic Potential of Over-the-Counter Agents >

Therapeutic & Toxic Potential of Over-the-Counter Agents

In the USA, drugs are divided by law into two classes: those restricted to sale by prescription only and those for which directions for safe use by the public can be written. The latter category constitutes the nonprescription or over-the-counter (OTC) drugs. In 2001, the American public spent approximately $18 billion on over 125,000 OTC products to medicate themselves for ailments ranging from acne to warts. These products contain approximately 1000 active ingredients in various forms and combinations.

It is apparent that many OTC drugs are no more than "me too" products advertised to the public in ways that suggest that there are significant differences between them. For example, there are over 100 different systemic analgesic products, almost all of which contain aspirin, acetaminophen, nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, or a combination of these agents as primary ingredients. They are made different from one another by the addition of questionable ingredients such as caffeine or antihistamines; by brand names chosen to suggest a specific use or strength ("women's," "migraine," "arthritis," "maximum"); or by special dosage formulations (enteric-coated tablets, geltabs, liquids, sustained-release products, powders, seltzers). There is a price attached to all of these features, and in most cases a less expensive generic product can be equally effective. It is probably safe to assume that the public is generally overwhelmed and confused by the wide array of products presented and will probably use those that are most heavily advertised.

Since 1972, the Food and Drug Administration (FDA) has been engaged in a methodical review of OTC ingredients for both safety and efficacy. There have been two major outcomes of this review:

(1) Ingredients designated as ineffective or unsafe for their claimed therapeutic use are being eliminated from OTC product formulations (eg, antimuscarinic agents have been eliminated from OTC sleep aids); and (2) Agents previously available by prescription only have been made available for OTC use because they were judged by the review panel to be generally safe and effective for consumer use without medical supervision (Table 64–1). Since the appointment of the Nonprescription Drugs Advisory Committee in 1993, the rate of switches from prescription to OTC status has accelerated. Indeed, more than 700 OTC products contain ingredients and dosages that were available only by prescription less than 30 years ago. Some agents such as docosanol and the nicotine polacrilex lozenge have bypassed the prescription route altogether and have been released directly to the OTC market. Other OTC ingredients previously available in low doses only are now available in higher-strength formulations. Examples of other prescription drugs currently under consideration for OTC reclassification include cyclobenzaprine, sucralfate, nonsedating antihistamines (cetirizine, fexofenadine), and topical penciclovir. The prescription to OTC reclassification process is very rigorous, and many agents have not been approved for OTC use. For example, the cholesterol-lowering agents cholestyramine, lovastatin, and pravastatin were denied OTC status on the basis that these agents could not be used safely and effectively in an OTC setting. The advisory committee believed that diagnosis and ongoing management by a health care provider was necessary for the management of hyperlipidemia, a chronic, asymptomatic condition with

potentially life-threatening consequences. In a similar recommendation, oral acyclovir for OTC use in the treatment of recurrent genital herpes was not approved because of concerns about misdiagnosis and inappropriate use leading to increased viral resistance.

Table 64–1. Selected Agents Switched from Prescription to Otc Status by the Food and Drug Administration.

1No single ingredient product available (brompheniramine/pseudoephedrine combination).

2No single ingredient product available (dexbrompheniramine/pseudoephedrine combination).

3Products containing phenylpropanolamine were withdrawn from the US market in 2000 based on reports of an increased risk of hemorrhagic stroke in patients using this agent.

4No single ingredient product available (triprolidine/pseudoephedrine combination).

There are three reasons why it is essential for clinicians to be familiar with this class of products. First, many OTC medications are effective in treating common ailments, and it is important to be able to help the patient select a safe, effective product. Because managed care practices encourage clinicians to limit the cost of drugs they prescribe, many will begin to recommend effective OTC treatments to their patients, since these drugs are rarely paid for by the insurance plan. (See Table

medical conditions or interact with prescription medications. (See Appendix II, Drug Interactions.) Finally, the misuse or abuse of OTC products may actually produce significant medical complications. Phenylpropanolamine, for example, a sympathomimetic previously found in many cold, allergy, and weight control products, was withdrawn from the United States market by the FDA in 2000 based on reports that the drug increased the risk of hemorrhagic stroke. A general awareness of these products and their formulations will enable clinicians to more fully appreciate the potential for OTC drug-related problems in their patients.

Table 64–2. Ingredients of Known Efficacy for Selected Over-the-Counter (OTC) Classes.