Transdermal preparations

Many systemically administered estrogen products are available in the United States, but conjugated equine estrogens (CEEs), prepared from the urine of pregnant mares, is the most widely prescribed. Transdermal estrogen preparations are also available and usually are prescribed for patients who experience adverse effects, elevated triglycerides, or liver function abnormalities while taking an oral product. Transdermal preparations also have a lower incidence of venous thromboembolism than oral preparations.9... 

The answer is e. (Hardmanr p 930.) All the drugs listed in the question are used as antiemetics. Chlorpromazine is a general antiemetic, used orally, rectally, or by injection for the control of nausea and vomiting that is caused by conditions that are not necessarily defined. Ondansetron is indicated in the oral or intravenous route for the prevention of nausea and vomiting caused by cancer chemotherapy Diphenhydramine and dimen-hydrinate are used orally for the active and prophylactic treatment of motion sickness. Scopolamine is a transdermal preparation used in the prevention of motion sickness. The drug is incorporated into a bandage-like... 

Nitroglycerin, the prototype of the nitrates is characterized by a rapid onset and short duration of action. It is usually administered sublingually (via the oro-mucosal route), which allows a rapid and efficient absorption and avoids the strong first pass effect after oral administration. Nitroglycerin is available as tablets, capsules (for sublingual administration) but also as transdermal preparations, sprays, and ointments. 

V.a.1.2. Transdermal preparations. Adhesive patches applied to the skin can be used to deliver oestrogens transdermally, using either a reservoir of liquid or an oestradiol-containing matrix. These systems deliver adequate amounts of oestradiol to maintain plasma levels within the normal range for 24 hours, and some preparations now provide transdermal progestagen also, thus avoiding the need for additional tablets to be taken for part of the cycle. 

Scopolamine is useful for prevention of motion sickness when the motion is very stressful and of short duration. A transdermal preparation (Transderm-Scop) with a 72-hour duration of action has been marketed for this purpose. Blockade of chohnergic sites in the vestibular nuclei and reticular formation may account for the effectiveness of this agent. When the motion is less stressful and lasts longer, the antihistamines (Hj-antagonists) are probably preferable to the antimus-... 

Increased skin temperature increases absorption rate of transdermal preparation... 

Clonidine 0.003-0.01 bid or tid Tourette s syndrome ADHD Aggression/self-abuse Severe agitation Withdrawal syndromes Sedation (very frequent) Hypotension (rare) Dry mouth Confusion (with high dose) Depression Rebound hypertension Localized irritation with transdermal preparation... 

Rebound hypertension Localized irritation with transdermal preparation Same as clonidine Less sedation, hypotension... 

The hepatic first-pass effect can be avoided to a great extent by use of sublingual tablets and transdermal preparations and to a lesser extent by use of rectal suppositories. Sublingual absorption provides direct access to systemic—not portal—veins. The transdermal route offers the same advantage. Drugs absorbed from suppositories in the lower rectum enter vessels that drain into the inferior vena cava, thus bypassing the liver. However, suppositories tend to move upward in the rectum into a region where veins that lead to the liver predominate. Thus, only about 50% of a rectal dose can be assumed to bypass the liver. 

A transdermal preparation of clonidine that reduces blood pressure for 7 days after a single application is also available. This preparation appears to produce less sedation than clonidine tablets but is often associated with local skin reactions. 

The accelerant should be suitable for formulation into topical and transdermal preparations, being compatible with drugs and excipients and promoting appropriate drug solubility in the formulation. 

The assay of transdermal preparations of scopolamine involve removing the polyester backing and extracting with chloroform at 60°C for 30 min [59]. Of the variety of different techniques evaluated for extracting triamcinolone acetonide in dermatological patches, liquid-liquid dispersion gave the best recovery and precision [60]. 

A small increase in the risk of gallbladder disease has been associated with the nse of HRT. Studies have shown that preparations containing oestrogen alone are associated with a greater risk than combination oestrogen/progestogen therapy. The formulation used is important, with transdermal preparations considered safer. 

Partitioning to the skin in the case of topical or transdermal preparations. 

One unusual variant involves appljfing a transdermal preparation to the scrotum (71), a technique that has been claimed to mimic more closely the natural pattern of release of endogenous testosterone. It is not clear that appljfing it at this site has any special merit, although some work suggests that the scrotal skin is less likely than other skin areas to exhibit local reactions. Certainly topical preparations of testosterone can elicit such reactions, with pruritus and bUster-ing being common, while induration, erythema, and allergic reactions can also occasionally occur. 

Ethanol and aqueous ethanol solutions of various concentrations (see Sections 8 and 17) are widely used in pharmaceutical formulations and cosmetics see Table 1. Although ethanol is primarily used as a solvent, it is also employed in solutions as an antimicrobial preservative. Topical ethanol solutions are also used as penetration enhancers " and as disinfectants. Ethanol has also been used in transdermal preparations in combination with Labrasol as a 7)... 

Included in the FDA Inactive Ingredients Guide (dental preparations inhalations IM, IV, and SC injections nasal and ophthalmic preparations oral capsules, solutions, suspensions, syrups, and tablets rectal, topical, and transdermal preparations). Included in the Canadian List of Acceptable Non-medicinal Ingredients. Included in nonparenteral and parenteral medicines licensed in the UK. 

Included in the FDA Inactive Ingredients Guide (transdermal preparation). Included in parenteral medicines licensed in the UK. Included in the Canadian List of Acceptable Non-medicinal Ingredients. 

Light mineral oil is used in applications similar to those of mineral oil. It is used primarily as an excipient in topical pharmaceutical formulations where its emollient properties are exploited in ointment bases see Table I. It is also used in ophthalmic formulations. Light mineral oil is additionally used in oil-in-water and polyethlylene glycol/gylcerol emulsions as a solvent and lubricant in capsules and tablets as a solvent and penetration enhancer in transdermal preparations and as the oily medium used in the microencapsulation of many drugs. ... 

The deliberate or accidental ingestion of belladonna alkaloids is a major cause of toxicity in humans. The most dangerous and spectacular manifestation of poisoning arises from the intense excitation of the central nervous system (CNS). Infants and young children are especially susceptible to the toxic effects of atropinic drugs. In adults, delirium or toxic psychoses without undue peripheral manifestations have been reported after instillation of atropine eye drops. Transdermal preparation of scopolamine has been reported to cause toxic psychoses, especially in children and in the elderly. Serious intoxication may occur in children who ingest berries or seeds containing... 

Use of hormone therapy for the management of vasomotor symptoms is cost-effective, and data to support the use of nonhormonal alternatives are limited. The cost of hormone therapy can vary depending on the route and method of delivery. Transdermal preparations are about twice as expensive as their equivalent oral preparations." Women who have undergone hysterectomy use hormone therapy more freqnently than do women with an intact uterus (58.7% versus 19.6%). ... 

Certain muscarinic antagonists are effective against motion sickness. They should be given pro-phylactically they are much less effective after severe nausea or vomiting has developed. Scopolamine is the most effective prophylactic agent for short (4—6 hours) exposures to severe motion, and probably for exposures of up to several days. A transdermal preparation of scopolamine (transderm scop) is highly effective when used prophylactically. Scopolamine, incorporated into a multilayered adhesive unit, is applied to the postauricular mastoid region, where transdermal... 

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