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

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Antifungal	Butenafine, 1%	Lotrimin Ultra	Effective for the treatment of
topical	(cream) apply to		tinea pedis (athlete's foot),
preparations	affected areas once		tinea cruris (jock itch), and
	daily		tinea corporis (ringworm).
			Clotrimazole and miconazole
	Clotrimazole, 1%	Lotrimin AF	Clotrimazole and miconazole
	Clotrimazole, 1%	Lotrimin AF	also effective against
	(cream, lotion,	Cream/Lotion/Solution,	also effective against
	solution), apply to	Mycelex OTC	Candida albicans.
	solution), apply to	Mycelex OTC
	affected areas twice
	daily

	Miconazole, 2%	Lotrimin AF
	(cream, powder,	Powder/Spray, Micatin,
	solution), apply to	Zeasorb-AF
	affected areas twice
	daily

	Terbinafine, 1%	Lamisil AT
	(cream), apply to
	affected areas once or
	twice daily

	Tolnaftate, 1% (cream,	Aftate, Tinactin, Ting,
	powder, solution),	various generic
	apply to affected areas
	twice daily

	Undecylenic acid, 10–	Cruex, Desenex, various
	25% (powder, spray	generic
	powder, cream, liquid)
	apply to affected areas
	twice daily
Antifungal	Butoconazole, 2%	Femstat-3, Mycelex-3	Topical vaginal antifungals
vaginal	cream, one		should only be used for
preparations	applicatorful		treatment of recurrent
	intravaginally at		vulvovaginal candidiasis
	bedtime for 3		previously diagnosed by a
	consecutive days		clinician in otherwise
			healthy, nonpregnant women.

	Clotrimazole (1%, 2%	Gyne-Lotrimin,	Insert one applicatorful (1%)
	vaginal cream, 100 mg,	Mycelex-7, Gyne-	or one tablet (100 mg)
	200 mg tablet); see	Lotrimin-3, various	intravaginally at bedtime for
	comments for dosage	generic	7 consecutive days.
			Alternatively: Insert one
			applicatorful (2%) or one
			tablet (200 mg),
			intravaginally at bedtime for
			3 consecutive days.

	Miconazole (2%, 4%	Monistat-7, Monistat-3	Insert one applicatorful
	vaginal cream; 100 mg,		intravaginally at bedtime for
	200 mg vaginal		7 consecutive days (2%) or 3
	suppositories); see		consecutive days (4%).
	comments for dosage		Alternatively: insert one

			suppository intravaginally at
			bedtime for 7 consecutive
			days (100 mg) or 3
			consecutive days (200 mg).

	Tioconazole, 6.5%	Monistat-1, Vagistat-1
	vaginal ointment, one
	applicatorful
	intravaginally at
	bedtime (single-dose)

Anti-	Hydrocortisone, 0.5%	Anusol HC, Cortaid,	Used to temporarily relieve
inflammatory	(cream, ointment,	Cortizone-5, Cortizone-	itching and inflammation
topical	lotion), 1% (cream	10, various generic	associated with minor rashes
preparations	ointment, lotion, spray)		due to contact or allergic
			dermatitides, insect bites, and
			hemorrhoids. Apply sparingly
			to affected areas two to four
			times daily.
Antiseborrheal	Coal tar, 0.5-15%	Denorex, Ionil T Plus,	Tar derivatives inhibit
agents	shampoo, dosage	Tegrin, Zetar, various	epidermal proliferation and
	varies; consult product	generic	may possess antipruritic and
	labeling		antimicrobial activity.

	Ketoconazole, 1%	Nizoral A-D	Synthetic azole antifungal
	shampoo, apply every		agent with activity versus
	3–4 days		Pityrosporum ovale, a fungus
			that may cause seborrhea and
			dandruff. Massage over entire
			scalp for 3 minutes. Rinse
			thoroughly and repeat
			application.
	Pyrithione zinc, 1–2%	Denorex, Head &	Both selenium sulfide and
	shampoo, apply once	Shoulders, Sebulon,	zinc pyrithione are cytostatic
	or twice weekly	various generic	agents that decrease
			epidermal turnover rates.
	Selenium sulfide, 1%	Head & Shoulders	epidermal turnover rates.
	Selenium sulfide, 1%	Head & Shoulders	Massage into wet scalp for 2–
	shampoo, apply once	Intensive Treatment,	Massage into wet scalp for 2–
	shampoo, apply once	Intensive Treatment,	3 minutes. Rinse thoroughly
	or twice weekly	Selsun Blue, various	3 minutes. Rinse thoroughly
	or twice weekly	Selsun Blue, various	and repeat application.
		generic	and repeat application.
		generic	Selenium sulfide can be
			Selenium sulfide can be
			irritating to the eyes and skin.

Antitussives	Codeine, 10–20 mg	Robitussin A-C, Guiatuss	Acts centrally to increase the
	every 4–6 hours (with	AC, various generic	cough threshold. In doses
	guaifenesin)		required for cough
			suppression, the addictive
			liability associated with
			codeine is low. Many
			codeine-containing
			antitussive combinations are
			schedule V narcotics, and
			OTC sale is restricted in
			some states.

	Dextromethorphan,	Benylin Adult Formula	Dextromethorphan is a
	10–20 mg every 4	Cough, Hold DM, Vicks	nonopioid congener of
	hours or 30 mg every	44 Cough Relief, various	levorphanol without
	6–8 hours	generic	analgesic or addictive
			properties. Often is used with
			antihistamines,
			decongestants, and
			expectorants in combination
			products.
Decongestants,	Oxymetazoline, 0.05%	Afrin, Dristan 12 Hour	Topical sympathomimetics
topical	nasal solution, 2–3	Nasal, Neo-Synephrine	are effective for the
	sprays per nostril every	12 Hour, various generic	temporary acute management
	10–12 hours		of rhinorrhea associated with
			common colds and allergies.
	Phenylephrine	Neo-Synephrine, various	common colds and allergies.
	(0.125%, 0.25%, 0.5%,	generic	Long-acting agents
	(0.125%, 0.25%, 0.5%,	generic	(oxymetazoline and
	1%), nasal solution, 2–		(oxymetazoline and
	1%), nasal solution, 2–		xylometazoline) are generally
	3 sprays/drops per		xylometazoline) are generally
	3 sprays/drops per		preferred, though
	nostril every 3–4 hours		preferred, though
	nostril every 3–4 hours		phenylephrine is equally

	Xylometazoline	Otrivin
	Xylometazoline	Otrivin	effective. Topical
	(0.05%, 0.1%), nasal		decongestants should not be
	solution, 2–3		used for longer than 3 days to
	sprays/drops per nostril		prevent rebound nasal
	every 8–10 hours		congestion.
			congestion.
Decongestants,	Phenylephrine, 10 mg	Novahistine Elixir,	Oral decongestants have a
systemic	every 4 hours	various generic	prolonged duration of action
		combination products	but may cause more systemic
			effects, including
	Pseudoephedrine, 60	Sudafed, various generic	effects, including
	mg every 4–6 hours or		nervousness, excitability,
	mg every 4–6 hours or		restlessness, and insomnia.
	120 mg (extended		restlessness, and insomnia.
	120 mg (extended		Also available in
	release) every 12 hours		Also available in
	release) every 12 hours		antihistamine, antitussive,
			antihistamine, antitussive,
			expectorant, and analgesic
			combination products.
			Phenylephrine is
			unpredictably absorbed from
			the gastrointestinal tract.

Expectorants	Guaifenesin, 100–400	Robitussin, various	The only OTC expectorant
	mg every 4 hours	generic	recognized as safe and
			effective by the FDA. Often
			used with antihistamines,
			decongestants, and
			antitussives in combination
			products.

Hair growth	Minoxidil, 2%, 5%	Rogaine for Men,	Minoxidil appears to directly
stimulants	solution, apply 1 mL to	Rogaine for Women,	stimulate hair follicles
	affected areas of scalp	Rogaine Extra Strength	resulting in increased hair
	twice daily.	for Men	thickness and reduced hair
			loss. Treatment for four

			months or longer may be
			necessary to achieve visible
			results. If new hair growth is
			observed, continued
			treatment is necessary as hair
			density returns to
			pretreatment levels within
			months following drug
			discontinuation.
Laxatives	Bulk formers:	Citrucel, Equalactin,	The safest laxatives for
	Polycarbophil,	Konsyl, Metamucil,	chronic use include the bulk
	psyllium and	Perdiem, various generic	formers and stool softeners.
	methylcellulose		Saline laxatives and
	preparations. Dosage		stimulants may be used
	varies; consult product		acutely but not chronically
	labeling		(see text). Bulk formers hold
			water and expand in stool,
			promoting peristalsis.

	Stool softeners:	Colace, Surfak, various	Soften fecal material via
	Docusate sodium, 50–	generic	detergent action that allows
	500 mg daily.		water to penetrate stool.
	Docusate calcium, 240
	mg daily

	Stimulant laxatives:	Correctol, Dulcolax, Ex-	Stimulant laxative actions
	Bisacodyl, 5–15 mg	Lax, Senokot, various	include direct irritation of
	daily. Senna: dosage	generic	intestinal mucosa or
	varies, consult product		stimulation of the myenteric
	labeling		plexus, resulting in
			peristalsis. These agents may
			also cause alteration of fluid
			and electrolyte absorption,
			resulting in luminal fluid
			accumulation and bowel
			evacuation.
Pediculicides	Permethrin 1%	Nix	Instructions for use varies;
(head lice)			consult product labeling.
(head lice)	Pyrethrins (0.3%)	A-200, RID	consult product labeling.
	Pyrethrins (0.3%)	A-200, RID	Avoid contact with eyes.
	combined with		Avoid contact with eyes.
	combined with		Comb out nits. Linens,
	piperonyl butoxide (3–		Comb out nits. Linens,
	piperonyl butoxide (3–		pajamas, combs, and brushes
	4%)		pajamas, combs, and brushes
	4%)		should be washed daily until
			should be washed daily until
			the infestation is eliminated.
			Repeat application 7 days
			later if live nits are still
			visible.

Sleep aids	Diphenhydramine, 25–	Compoz, Nytol,	Diphenhydramine and
	50 mg at bedtime	Sominex, various generic	doxylamine are

			may be indicative of a serious
			underlying condition
			requiring medical attention,
			patients should consult a
			physician if insomnia persists
			continuously for longer than
			2 weeks.
Smoking	Nicotine (transdermal	Nicoderm CQ, Nicotrol,	Nicotine replacement
cessation aids	patch), dosage varies;	various generic	products in combination with
	consult product		behavioral support
	labeling		approximately double
			abstinence rates compared to
	Nicotine polacrilex	Nicorette, Commit,	abstinence rates compared to
	Nicotine polacrilex	Nicorette, Commit,	placebo. Review directions
	gum or lozenge;	various generic	placebo. Review directions
	gum or lozenge;	various generic	for use carefully, since
	dosage varies; consult		for use carefully, since
	dosage varies; consult		product strengths vary and
	product labeling		product strengths vary and
	product labeling		self-titration and tapering
			self-titration and tapering
			may be necessary.

Table 64–2 lists examples of OTC products that may be used effectively to treat common medical problems. The selection of one ingredient over another may be important in patients with certain medical conditions or in patients taking other medications. These are discussed in detail in other chapters. The recommendations listed in Table 64–2 are based upon the efficacy of the ingredients and on the principles set forth in the following paragraphs.

(1)Select the product that is simplest in formulation with regard to ingredients and dosage form. In general, single-ingredient products are preferred. Although some combination products contain effective doses of all ingredients, others contain therapeutic doses of some ingredients and subtherapeutic doses of others. Furthermore, there may be differing durations of action among the ingredients, and there is always a possibility that the clinician or patient will be unaware of the presence of certain active ingredients in the product. Acetaminophen, for example, is present in many cough and cold preparations; a patient unaware of this may take separate doses of analgesic in addition to that contained in the cold preparation, potentially leading to toxicity.

(2)Select a product that contains a therapeutically effective dose.

(3)Carefully read the product labeling to determine which ingredients are appropriate based on the patient's symptoms and underlying health conditions and whatever is known about the medications the patient is already taking.

(4)Recommend a generic product if one is available.

(5)Be wary of "gimmicks" or advertising claims of specific superiority over similar products.

(6)For children, the dose, dosage form, and palatability of the product will be prime considerations.

Certain ingredients in OTC products should be avoided or used with caution in selected patients

patient is taking. Many of the more potent OTC ingredients are hidden in products where their presence would not ordinarily be expected (Table 64–3). While most OTC medications are clearly labeled with the specific ingredients contained in the product, many products do not presently conform to the new FDA-mandated standardized OTC medication labeling requirements that are being phased in through 2005. Lack of awareness of the ingredients present in OTC products and the belief by many physicians that OTC products are ineffective and harmless may cause diagnostic confusion and perhaps interfere with therapy. For example, innumerable OTC products, including analgesics and allergy, cough, and cold preparations, contain sympathomimetics. These agents should be avoided or used cautiously by type 1 diabetics and patients with hypertension, angina, or hyperthyroidism. Aspirin should not be used in children and adolescents for viral infections (with or without fever) because of an increased risk of Reye's syndrome. Aspirin and other NSAIDs should be avoided by individuals with active peptic ulcer disease, certain platelet disorders, and patients taking oral anticoagulants. Cimetidine, an H2-receptor antagonist, is a well-known inhibitor of hepatic drug metabolism and can increase the blood levels and toxicity of drugs such as phenytoin, theophylline, and warfarin.

Table 64–3. Hidden Ingredients in Over-the-Counter (OTC) Products.

Hidden Drug or Drug	OTC Class Containing	Product Examples
Class	Drug
Alcohol (percent ethanol)	Cough syrups, cold	Cheracol Plus (5%)
	preparations	Comtrex Multi-Symptom Cold &
	preparations

		Cough Relief (10%)
		Vicks 44M (10%)
		Vicks 44M (10%)
		Vicks NyQuil Liquid (10%)
		Vicks NyQuil Liquid (10%)
	Mouthwashes	Cepacol Mouthwash (14%)
		Listerine (27%)
		Listerine (27%)
		Scope (15%)
		Scope (15%)
Antihistamines	Analgesics	Aspirin Free Anacin PM
		Aspirin Free Excedrin PM
		Aspirin Free Excedrin PM
		Extra Strength Bayer PM
		Extra Strength Bayer PM
		Percogesic Extra Strength
		Percogesic Extra Strength
		Tylenol PM
		Tylenol PM
		Tylenol Severe Allergy
		Tylenol Severe Allergy
	Menstrual products	Midol PM
		Maximum Strength Midol Menstrual
		Maximum Strength Midol Menstrual
		Maximum Strength Midol PMS
		Maximum Strength Midol PMS
		Maximum Strength Multi-Symptom
		Maximum Strength Multi-Symptom
		Pamprin
		Menstrual Relief
		Menstrual Relief
		Premsyn PMS
		Premsyn PMS

	Sleep aids	Compoz

		Nytol
		Sominex
		Twilite Caplets
		Unisom
Aspirin and other	Antidiarrheals	Pepto-Bismol (bismuth subsalicylate)
salicylates	Cold/allergy preparations	Alka-Seltzer Plus Cold & Cough
	Cold/allergy preparations	Alka-Seltzer Plus Cold & Cough
		Liqui-Gels
		BC Allergy Sinus Cold Powder
Caffeine	Analgesics	Alka-Seltzer Morning Relief
		Anacin
		Cope
		Excedrin Extra Strength
		Excedrin Migraine
		Goody's Extra Strength Fast Relief
		Goody's Extra Strength Headache
		Powder
		Vanquish

	Menstrual products	Maximum Strength Midol Menstrual
	Stimulants	Lucidex
		NoDoz
		Vivarin
Local anesthetics (usually	Antitussives/Lozenges	Cepacol Maxium Strength Lozenges
benzocaine)		Spec T Sore Throat/Cough
		Spec T Sore Throat/Cough
		Suppressant
		Vicks Chloraseptic Lozenges
	Dermatologic preparations	Americaine
		Bactine
		Dermoplast
		Lanacane
		Solarcaine
	Hemorrhoidal products	Americaine
		Anusol Ointment
		Medicone
		Tronolane
	Toothache, cold sore, and	(Many)
	teething products	Anbesol
		Anbesol
		Baby Orajel
		Kank-A

		Orabase B
		Zilactin-B
Sodium (mg/tablet or mg/5	Analgesics	Alka-Seltzer Original Effervescent
mL or as stated)		Tablet (568)
		Alka-Seltzer Extra Strength
		Effervescent Tablet (588)
		Bromo-Seltzer Granules (959/pre-
		measured packet)
	Antacids	Alka-Seltzer Original Effervescent
		Tablet (568)
		Alka-Seltzer Extra Strength
		Effervescent Tablet (588)
		Alka-Seltzer Gold (299)
		Alka-Seltzer Heartburn Relief (569)
		Bromo-Seltzer Granules (959/pre-
		measured packet)
		Citrocarbonate Effervescent Granules
		(780/ teaspoon)
	Laxatives	Fleets Enema (4,439 mg, of which
		275–400 mg/enema is absorbed)
		Fleet Phospho-Soda (554/teaspoon)
Sympathomimetics	Analgesics	Motrin Sinus Headache
		Sinarest No Drowsiness
		Sine-Aid Sinus Headache Tablets
		Sinutab
		Tylenol Flu Day Non-Drowsy
		Tylenol Sinus Day Non-Drowsy
	Asthma products	Bronkaid Dual Action
		Primatene
	Cold/allergy preparations	(Many)
		Advil Cold and Sinus
		Alka-Seltzer Plus
		Comtrex Maximum Strength Day and
		Night Flu
		Contac Severe Cold and Flu
		Dimetapp Cold & Allergy
		PediaCare Cold & Allergy
		Motrin Cold & Flu
		Sudafed
		TheraFlu Severe Cold & Congestion

				Triaminic Chest Congestion
				Vicks 44M
				Vicks DayQuil
				Vicks NyQuil
	Cough preparations			(Many)
				PediaCare Long Lasting Cough Plus
				Cold
				Robitussin PM Cold & Cough
				Robitussin Maximum Strength
				Cough & Cold
				Triaminic Cough
				Vicks 44D
	Hemorrhoidal products			Hem-Prep
				Pazo Hemorrhoid Ointment
				Preparation H

	Sore throat products			Spec-T Sore Throat/Decongestant

Overuse or misuse of OTC products may induce significant medical problems. A prime example is rebound congestion from the regular use of decongestant nasal sprays for more than 3 days. The improper and chronic use of some antacids (eg, aluminum hydroxide) may cause constipation and even impaction in elderly people, as well as hypophosphatemia. Laxative abuse can result in abdominal cramping and fluid and electrolyte disturbances. Insomnia, nervousness, and restlessness can result from the use of sympathomimetics or caffeine hidden in many OTC products (Table 64– 3). The chronic systemic use of some analgesics containing large amounts of caffeine may produce rebound headaches, and long-term use of analgesics has been associated with interstitial nephritis. Recent evidence suggests that use of OTC products containing aspirin, other salicylates, acetaminophen, ibuprofen, naproxen, or ketoprofen may increase the risk of hepatotoxicity and gastrointestinal hemorrhage in individuals who consume three or more alcoholic drinks daily. Furthermore, acute ingestion of large amounts of aspirin or acetaminophen by adults or children can cause serious toxicity. Antihistamines may cause sedation or drowsiness, especially when taken concurrently with sedative-hypnotics, tranquilizers, alcohol, or other central nervous system depressants. Finally, antihistamines, local anesthetics, antimicrobial agents, counterirritants, p- aminobenzoic acid (PABA) and preservatives contained in a myriad of OTC topical and vaginal products may induce allergic reactions.

There are three major drug information sources for OTC products. Handbook of Nonprescription Drugs is the most comprehensive resource for OTC medications; it evaluates ingredients contained in major OTC drug classes and lists the ingredients included in many OTC products. Nonprescription Drug Therapy is a loose-leaf reference, updated quarterly, that provides detailed OTC product information and patient counseling instructions. Physicians' Desk Reference for Nonprescription Drugs, a compendium of manufacturers' information regarding OTC products, is published annually but is somewhat incomplete with regard to the number of products included and the consistency of information provided. Any health care provider who seeks more specific information regarding OTC products may find the references useful.

Chapter 65. Botanicals ("Herbal Medications") & Nutritional

Supplements

Botanicals ("Herbal Medications") & Nutritional Supplements: Introduction

The medical use of botanicals in their natural and unprocessed form undoubtedly began when the first intelligent animals noticed that certain food plants altered particular body functions. Much information exists about the historical use and effectiveness of botanical products. Unfortunately, the quality of this information is extremely variable. One of the most complete compendiums of clinical recommendations regarding the use of botanicals is the Report of the German Commission E (a committee that sets standards for herbal medications in that country; Blumenthal, 2000). Interest in the endocrine effects and possible nutritional benefits of certain purified chemicals such as dehydroepiandrosterone, melatonin, high-dose vitamins, and minerals has led to a parallel development of consumer demand for such substances. These substances, together with the botanicals, constitute a substantial source of profits for those who exploit the concept of "alternative medicine."

The alternative medicinal substances are distinguished from similar botanical substances used in traditional medicine (morphine, digitalis, atropine, etc) by virtue of being available without a prescription and, unlike over-the-counter medications, being legally considered dietary supplements rather than drugs (thus avoiding conventional FDA oversight). Among the purified chemicals, dehydroepiandrosterone and melatonin are of significant pharmacologic interest.

This chapter provides an evidence-based approach to the pharmacology and clinical efficacy of several of the commonly used and commercially available botanicals and dietary supplements. Ephedrine, the active principle in Ma-huang, is discussed in Chapter 9: Adrenoceptor-Activating & Other Sympathomimetic Drugs.

Regulatory Factors

Dietary supplements (which include vitamins, minerals, cofactors, herbal medications, and amino acids) are not considered over-the-counter drugs in the USA but rather food supplements. In 1994, the United States Congress, influenced by growing "consumerism" as well as strong manufacturer lobbying efforts, passed the Dietary Supplement and Health Education Act (DSHEA). This landmark act prevented adequate FDA oversight of these substances. Thus, DSHEA has allowed a variety of substances with pharmacologic activity—if classified as dietary supplements—to be sold without a prescription or any FDA review of efficacy or safety prior to product marketing. Dietary supplements are governed under Current Good Manufacturing Practice in Manufacturing, Packaging or Holding Human Food (CGMP) regulations. Although administered by the FDA, CGMP regulations are often inadequate to ensure product purity, potency, and other variables such as accurate product identification and appropriate botanical harvesting. Therefore, much of the criticism regarding the dietary supplement industry involves a lack of product purity and variations in potency.

In 1999, the FDA announced labeling recommendations for dietary supplements marketed in the USA. These recommendations were not mandated; some manufacturers, however, have adopted them in an effort to increase sales. According to these recommendations, the term "dietary

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