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Although the binding proteins (cytophilins) Azathioprine is well absorbed following oral adminis- for cyclosporine and tacrolimus are different spasms near anus cheap generic mestinon uk, they share tration infantile spasms 7 month old purchase mestinon 60 mg with amex, with peak blood levels occurring within 1 to 2 similar functions in that the cytophilins are important hours spasms and spasticity trusted mestinon 60mg. It is speculated mercaptopurine, which is further converted in the liver that these proteins are important in regulating gene ex- and erythrocytes to a variety of metabolites, including 6- pression in T lymphocytes and that both drugs some- thiouric acid. Although its beneficial effect in various condi- Sirolimus tions is principally attributable to its direct immunosup- pressive action, the antiinflammatory properties of the Sirolimus (Rapamune) is structurally related to drug play an important role in its overall therapeutic ef- tacrolimus. This mechanism of action is different it is usually reserved for patients who do not respond to from those of tacrolimus and cyclosporine. It has largely been replaced by cyclosporine in im- Azathioprine (Imuran) is a cytotoxic agent that prefer- munosuppressive therapy. Since im- agents, the better oral absorption of azathioprine is the munologically competent cells are generally rapidly di- reason for its more widespread clinical use. The therapeutic use of azathioprine has been limited by Azathioprine, in combination with corticosteroids, the number and severity of adverse effects associated has historically been used more widely than any other with its administration. It is classified as a sulting in leukopenia, thrombocytopenia, or both may 57 Immunomodulating Drugs 661 occur. Because of its immunosuppressive activity, been used successfully alone and in combination with azathioprine therapy can lead to serious infections. It azathioprine and corticosteroids to prevent renal allo- has been shown to be mutagenic in animals and humans graft rejection. Mycophenolate Mofetil Antithymocyte globulin binds to circulating T lym- phocytes in the blood, which are subsequently removed Mycophenolate mofetil (CellCept), in conjunction with from the circulation by the reticuloendothelial system. It is used steroids is a more effective regimen than azathioprine for the prevention of acute allograft rejection in kid- in preventing the acute rejection of transplanted organs. It is also used to deplete T cells in marrow from donors before bone marrow transplanta- Other Cytotoxic Drugs tion. See Chapter 56 for izing antibodies may develop over time and necessitate further details of these agents. Antibodies Antiserum can be raised against lymphocytes or thymo- Rho(D) Immune Globulin cytes by the repeated injection of human cells into an An Rh-negative mother can become sensitized to Rh appropriate recipient, usually a horse. This antiserum or the immune globulin fraction derived sensitization may lead to Rh hemolytic disease in future from it has been used to produce immunosuppression. Rho(D) graft systems, the responses are variable, particularly immune globulin functions to prevent the mother from from one batch of serum to another. It is generally given at 28 weeks of pregnancy Antithymocyte globulin (Atgam) is purified immune and within 72 hours after delivery. Rh incompatibility globulin obtained from hyperimmune serum of horses can be identified with routine blood tests. These conditions humoral immunodeficiency, congenital agammaglobu- include immunodeficiency diseases, cancer, some types linemias, common variable immunodeficiency, severe of viral and fungal infections, and certain autoimmune combined immunodeficiency, idiopathic thrombocy- disorders. Immunostimulating agents are nonspecific; they cause The principal side effects are possible anaphylactoid general stimulation of the immune system. In most cases, the pharmacol- Thymic factors are naturally occurring substances that ogy of these agents has not been well described. The most promote T-lymphocyte differentiation and differentia- commonly used agents are discussed next. Nonviable strains of the thymic factors are used to enhance T-lymphocytic func- bacterium also have been shown to augment the im- tions. Studies with thymodulin show appears to stimulate natural killer cells, which in turn promise in treating symptoms in asthmatics and pa- can kill malignant cells. It is instilled directly into Few major side effects have been reported, espe- the bladder, where it is held for 2 hours before urination. An exciting application of immunomodulating therapy Levamisole is in the use of cytokines (lymphokines, monokines). As mentioned earlier in this chapter, immune cell function Levamisole (Ergamisol) was originally developed as an is regulated by cytokines produced by leukocytes or antihelminthic drug (see Chapter 54). With the advent of genetic engi- stimulatory effects of antigens, mitogens, lymphokines, neering, cytokines can be produced in pure form and in and chemotactic factors on lymphocytes, granulocytes, large quantities. It also can induce B-lymphocyte prolifera- either from donors in the general population or from tion, activate macrophage activity, and augment the hyperimmunized donors.

Rounding this dose to an amount available as an oral dosage form spasms diaphragm hiccups buy genuine mestinon, 1200 mg of lithium carbonate would be given every 12 hours spasms 1983 dvd mestinon 60mg free shipping. Upon initiation of therapy muscle relaxant and anti inflammatory 60 mg mestinon with mastercard, serum concentrations can be measured every 2–3 days for safety reasons in patients that are predisposed to lithium toxicity even though steady state has not yet been achieved. Once the desired steady-state lithium concen- tration has been achieved, lithium concentrations should be rechecked every 1–2 weeks for approximately 2 months or until concentrations have stabilized. Using linear pharmacokinetics, the new dose to attain the desired concentration should be proportional to the old dose (1200 mg/d) that produced the measured con- centration: Dnew = (Css,new/Css,old)Dold = (0. When lithium dosage alterations are needed, lithium serum concentrations should be measured within 1–2 weeks after the change. During lithium maintenance therapy, steady-state lithium serum concentrations should be repeated every 3–6 months. This time period should be altered to every 6–12 months for patients whose mood is stable or every 1–2 months for patients with frequent mood alterations. Enter patient’s demographic, drug dosing, and serum concentration/time data into the computer program. The pharmacokinetic parameters computed by the program are a volume of distribu- tion of 112 L, a half-life equal to 35 hours, and a clearance equal to 2. The one-compartment first-order absorption equations used by the program to com- pute doses indicates that a dose of 21 mmol Li+ every 12 hours will produce a steady- state concentration of 0. Rounding this dose to an amount available as an oral dosage form, 750 mg of lithium carbonate would be given every 12 hours. When lithium dosage alterations are needed, lithium serum concentrations should be measured within 1–2 weeks after the change. During lithium maintenance therapy, steady-state lithium serum concentrations should be repeated every 3–6 months. This time period should be altered to every 6–12 months for patients whose mood is stable or every 1–2 months for patients with frequent mood alterations. The doses would be given at 0900 H, 1500 H, and 2100 H to allow a 12-hour window after the evening dose so that lithium serum concentration measurements can be made. Upon initiation of therapy, serum concentrations can be measured every 2–3 days for safety reasons in patients that are predisposed to lithium toxicity even though steady state has not yet been achieved. Once the desired steady-state lithium concen- tration has been achieved, lithium concentrations should be rechecked every 1–2 weeks for approximately 2 months or until concentrations have stabilized. Enter patient’s demographic, drug dosing, and serum concentration/time data into the computer program. The pharmacokinetic parameters computed by the program are a volume of distribution of 44 L, a half-life equal to 25 hours, and a clearance equal to 1. The one-compartment first-order absorption equations used by the program to com- pute doses indicates that a dose of 8 mmol Li+ every 8 hours will produce a steady- state concentration of 0. Rounding this dose to an amount available as an oral dosage form, 300 mg of lithium carbonate would be given at 0900 H, 1500 H, and 2100 H to allow a 12 hours window after the evening dose so that lithium serum concentration measure- ments can be made. Upon initiation of therapy, serum concentrations can be measured every 2–3 days for safety reasons in patients that are predisposed to lithium toxicity even though steady state has not yet been achieved. Once the desired steady-state lithium concen- tration has been achieved, lithium concentrations should be rechecked every 1–2 weeks for approximately 2 months or until concentrations have stabilized. Using linear pharmacokinetics, the new dose to attain the desired concentration should be proportional to the old dose (1800 mg/d) that produced the measured con- centration: Dnew = (Css,new/Css,old)Dold = (1 mmol/L / 1. When lithium dosage alterations are needed, lithium serum concentrations should be measured within 1–2 weeks after the change. During lithium maintenance therapy, steady-state lithium serum concentrations should be repeated every 3–6 months. This time period should be altered to every 6–12 months for patients whose mood is stable or every 1–2 months for patients with frequent mood alterations. Enter patient’s demographic, drug dosing, and serum concentration/time data into the computer program.

Tolerance associated with renal retention of fluid and diltiazem undergo greater first-pass metabolism rel- does not occur; an initial natriuretic effect is often ative to nifedipine spasms hands fingers safe 60 mg mestinon, resulting in lower bioavailability of observed muscle relaxant eperisone discount mestinon 60mg with visa, especially with the nifedipine group of the former two drugs muscle relaxant non prescription proven mestinon 60 mg. They do not have significant effects on the re- verapamil and diltiazem, whose metabolites have phar- lease of renin or cause long-term changes in lipid macological activity. Postural hypotension, first-dose effect, and re- thus requiring higher plasma concentrations after oral bound phenomenon are not commonly seen. Their use is generally contraindicated in obstruc- dizziness, facial flushing, hypotension, and so forth. No consistent or doses of verapamil in elderly patients are known to significant changes in lipid and glucose levels have been cause constipation. Non–sustained release lowing the intravenous use of verapamil, include formulations of nifedipine are contraindicated in hyper- marked negative inotropic effects and depression of tension because of sympathetic rebound that may ag- preexisting sick sinus syndrome,A-V nodal disease, and gravate existing left ventricular dysfunction. The three pro- (A) Their interaction with membrane phospho- totypes, verapamil, nifedipine, and diltiazem, act at lipids results in a nonselective decrease of ion trans- three discrete sites at this channel. The other three drugs (dihydropyridines) are (B) They inhibit the Na –Ca exchanger in car- characterized by relatively selective vasodilator ef- diac and smooth muscle. The vasodilatory effects of nifedipine are largely (D) Their interaction with the sodium pump results restricted to arteries (and consequently the after- in an inhibition of calcium transport. Skeletal muscles depend on the mobilization of (B) Verapamil intracellular stores of calcium for their contractile (C) Nicardipine responses rather than transmembrane flux of cal- (D) Amlodipine cium through the calcium channels. All of the following statements regarding the phar- calcium channel blocker drugs: An up-to-date per- macokinetics of calcium channel blockers are cor- spective on the proposed hazards. Mechanisms of action of calcium channel (C) Their half-life is not altered by hepatic cirrho- antagonists. He sustained release, is characterized by relatively occasionally has angina precipitated by physical rapid onset of vasodilatory effects. This man’s side exertion and rapidly controlled by sublingual use of effects reflect the rapid and intense fall in blood nitroglycerin. He also is a result of drug-induced periodic increases in develops flushing, dizziness, and nervousness shortly heart rate. It is estimated that in the to the recommendations of the Sixth Joint National United States, as many as 60 million people are hyper- Committee on the Detection, Evaluation, and Treat- tensive or are being treated with antihypertensive ment of High Blood Pressure. Among the growing population of elderly ered to be stage I, or mild, if diastolic pressure is 90 to Americans, some 15 million have high blood pressure. Since in general terms hypertension can be de- ber of factors, including the patient’s age, sex, race, and fined as the level of blood pressure at which there is lifestyle. As a working definition, many cardiovascular risk, the ultimate judgment concerning the severity of treatment centers consider that a diastolic pressure of hypertension in any given individual must also include 90 mm Hg or higher or a systolic pressure of 140 mm Hg a consideration of factors other than diastolic or systolic or higher represents hypertension. In this situation, the loop tension is secondary to a known organic disease, such as diuretics furosemide and bumetanide are recom- renovascular disease or pheochromocytoma, therapy is mended; they have greater intrinsic natriuretic potency directed toward correction of the underlying malady. The therapy of primary, or essen- In situations of known renin–angiotensin–aldos- tial hypertension, as these cases are generally called, is terone involvement, such as in hypertension secondary often empirical. The K -sparing action of spironolactone, tri- The second employs drugs that interfere with the amterene, and amiloride serves as the basis for their oc- renin–angiotensin system, and the third is aimed at a casional use in the therapy of primary hypertension. A reduction in peripheral types of diuretics to help alleviate the K loss caused by vascular resistance can be achieved directly by relaxing them. Under these conditions, K balance is improved vascular smooth muscle with drugs known as vasodila- while natriuresis is maintained. Other chapters offer additional information on diuretics (see Chapter 21), the renin– The drugs discussed in this section produce a direct re- angiotensin system (see Chapter 18), adrenergic recep- laxation of vascular smooth muscle and thereby their tor antagonists (see Chapter 11), and the calcium chan- actions result in vasodilation. The exact mechanisms by which diuretics lower blood The vasodilators decrease total peripheral resistance pressure are not entirely understood. Initially, diuretics and thus correct the hemodynamic abnormality that is produce a mild degree of Na depletion, which leads to responsible for the elevated blood pressure in primary a decrease in extracellular fluid volume and cardiac hypertension. The effectiveness of diuretic therapy in mild vascular smooth muscle, the vasodilators are effective in hypertension may also involve either interference with lowering blood pressure, regardless of the etiology of or blunting of cardiovascular reflexes. Unlike many other antihypertensive the details, there is general agreement that the blood agents, the vasodilators do not inhibit the activity of pressure–lowering effects of diuretics do ultimately de- the sympathetic nervous system; therefore, orthostatic pend on the production of diuresis.

Breast fect of progesterone on endometrial cancer is not cancer occurs in both premenopausal and postmeno- known muscle relaxant sciatica mestinon 60 mg otc. Other clinical uses of estrogens and progestins include Mild hypertension and fluid retention frequently oc- the treatment of dysfunctional uterine bleeding muscle relaxant 2631 generic mestinon 60mg amex, dys- cur in oral contraceptive users spasms falling asleep safe 60 mg mestinon. Systolic blood pressure menorrhea, endometriosis, and rarely, metastatic pros- is elevated 5 to 6 mm Hg; diastolic blood pressure in- tate cancer. Hypertension is not commonly a problem in postmenopausal women Breast Cancer receiving conjugated estrogens. Migraine headaches (conjugated equine estrogens plus medroxyproges- may be a warning signal for an oncoming stroke, and terone acetate) compared with women taking estrogen immediate discontinuation of oral contraceptive use is alone (conjugated equine estrogens). Thus, the ability of progestins to Teratogenesis protect the endometrium from cancer risk is not ob- served in breast tissue. An increased Oral contraceptive use lessens the incidence of ovarian cancer incidence in male offspring of mothers who had cancer. Therefore, if pregnancy is sus- pected, oral contraceptive use should not be initiated or Hepatocellular carcinoma and benign hepatomas are use should be stopped promptly. Fertility Cardiovascular Complications There is some delay in the return of fertility after dis- continuation of oral contraceptive use. Gonadotropin Estrogen replacement therapy is associated with an in- profiles should be normal 3 months after combination creased risk of thromboembolic disease, and alternative oral contraceptive use is stopped. The incidence of pro- therapies for osteoporosis and cardiovascular protec- longed amenorrhea extending beyond 6 months is 2 to tion are recommended for individuals with prior throm- 3%. Breast Feeding These preparations alter liver function more signifi- cantly than do the natural estrogens, such as the sulfate The use of oral contraceptives may interfere with lacta- conjugates or esterified estrogens. In addition, the hormones may be present in the synthesis of specific liver proteins, such as coagulation mother’s milk, hence be taken in by the nursing child. If factors and fibrinogen, are implicated in the formation breast feeding is planned, the use of oral contraceptives of thromboembolisms. Gallbladder Disease Current estimates are that oral contraceptive use doubles to triples the overall risk of thromboembolic There is a 2. At very high doses, generally Estrogen usage is associated with a mild decrease in no longer used in cancer treatment, ocular toxicity has glucose tolerance. There is a slight risk of hepatocellular their concurrent use in the diabetic patient may neces- carcinoma in humans receiving long-term (5 years) ta- sitate adjustment in insulin dosage. This reaction is generally regarded to neomycin, penicillin V, chloramphenicol, sulfonamides, be a premalignant state, because individuals reported nitrofurantoin, phenytoin, barbiturates, primidone, to have endometrial hyperplasia later have a higher analgesics, and phenothiazines. The oral contraceptives also may decrease the effec- Administration of estrogens only is associated with a 1. Women receiving progestins 10 days per in hepatic microsomal drug-metabolizing enzymes, month during estrogen therapy generally do not de- competition for binding sites on plasma proteins, and velop endometrial carcinoma. The occurrence of multiple births fol- lowing ovulation induction with clomiphene is 4 to 9%; Formulation 90% of these multiple births are twins. Since clo- Estrogens Breast or endometrial cancer or vaginal miphene is teratogenic, therapy should be discontinued bleeding of unknown origin if there is a chance that conception has occurred. Pregnancy Rarely, irreversible ocular toxicities have been reported Hepatic dysfunction or liver cancer Preexisting cardiovascular disease with clomiphene use. Progestins Pregnancy Nausea, vomiting, and hot flashes may accompany Depression tamoxifen administration. Tamoxifen may cause a tran- Oral contraceptives Pregnancy sient flare of tumor growth and increased pain due to Smokers over age 35 bone metastases. These reactions are thought to be due Antiestrogens Pregnancy Endometrial cancer to an initial estrogenic action of this drug. Although progestin-only oral contraceptive for- (A) Estrogen only mulations are available, the combination of estro- (B) Progestin only gen and progestin is considered the safest and most (C) Combination of estrogen and progestin desirable type. Estrogen therapy is contraindicated in the pres- tion of estrogen and progestin should be consid- ence of breast cancer. The use of estrogen replacement for ing menopause but that she does not want to take short periods (up to 2 years) is not associated with any hormones because her mother had breast can- an increased incidence of breast cancer. You should cer and she was afraid that this would increase her also point out that osteoporosis is the most serious risk.

There are many molecule that stimulates leukocyte activation spasms stomach order genuine mestinon online, bone ways to get around this problem spasms sleep order mestinon 60mg with amex, including supposi- reabsorption muscle relaxant apo 10 purchase mestinon pills in toronto, and cartilage degradation. In rheumatoid arthritis, these effects include It is used in the treatment of myasthenia gravis and bone and cartilage destruction in the joints. Infammation, Immune Pharmacology, and Toxicology 271 (E) Pilocarpine is used in the treatment of glaucoma. This results in the accumu- lation of acetaldehyde in the blood, causing fushing, 22 The answer is A: Blockade of adenosine receptors. Disulfram Several mechanisms have been proposed for the has found some use in the patient seriously desiring actions of methylxanthines, including translocation of to stop alcohol ingestion. A conditioned avoidance extracellular calcium, increase in cyclic adenosine response is induced so that the patient abstains monophosphate and cyclic guanosine monophos- from alcohol to prevent the unpleasant effects of phate caused by inhibition of phosphodiesterase, and disulfram-induced acetaldehyde accumulation. Ototoxicity, which acting opiate antagonist that should be used in con- often presents as tinnitus, is a known side effect of junction with supportive psychotherapy. This is especially is better tolerated than disulfram and does not pro- true when given with other ototoxic drugs (such as duce the aversive reaction that disulfram does. It may aminoglycoside antibiotics), in patients with renal work well in this patient who had diffculty taking disease, when given in high doses, or with rapid intra- aldehyde dehydrogenase. Chelating agents are which normally causes sodium reabsorption in the (usually) organic compounds that can form multiple distal tubule. However, this agent has numerous undesirable side 25 The answer is C: Inhibits conversion of lanosterol to effects (such as anticholinergic effects) that it is less ergosterol. Sporothrix and other 272 Chapter 7 fungi stabilize their cell membranes with ergosterol not caused by an oxygen–hemoglobin concentration (which is not found in humans) in the same way that defcit. The short itraconazole inhibit a fungal cytochrome P450 enzyme duration of anesthetic action is caused by the decrease responsible for the last step in ergosterol synthesis: of barbiturate concentration in the brain to a level conversion of lanosterol to ergosterol. These and amphotericin B are examples of antifungals that drugs may remain in the body for relatively long peri- disrupt the fungal cell membrane by binding ergos- ods of time after their administration, because only terol and causing pore formation. Itraconazole does about 15% of the dose of barbiturates entering the not lead to membrane pore formation. Itraconazole does not inhibit squalene monooxygen- 29 The answer is B: Improved intestinal circular muscle ase. Overall, mor- phine and other narcotics produce constipation, with 26 The answer is B: Hepatic necrosis. There are toxic reactions combination of the stool softener docusate with the that some patients (especially females) develop after stimulant laxative senna has been used successfully to halothane anesthesia. To avoid this condition, halo- thane anesthesia is not repeated at intervals of less 30 The answer is B: Constipation. Physical and psychological dependence readily occur with morphine and with some of the other agonists. Recent investi- order elimination, meaning the same amount is gations have identifed a dramatic increase in the eliminated per unit time regardless of its concentra- myoplasmic calcium ion concentration. Ligand-gated membrane of drug are eliminated when their blood concen- channel is modulated by inhaled anesthetics. The duration of frst-order type (A) Malignant hyperthermia is not a drug toxicity drugs is therefore explained by their half-life or the event. This scenario describes a latter are known to inhibit drug metabolism, leading case of malignant hyperthermia. Most prolongation is more common than myocardial in- cases involve a mutated ryanodine receptor and are farction in this setting. With chronic believed to inhibit calcium release from the sarcoplas- use, procainamide causes a high incidence of side mic reticulum. By paralyzing the muscle in this way, effects, including a reversible lupus erythematosus– muscle cell metabolism is drastically decreased. It can be used for mild pain and fevers but is not cause asystole or induction of ventricular arrhyth- useful in malignant hyperthermia. Neuroleptic malignant (A) This patient has no evidence to suggest contact syndrome in some ways resembles malignant hyper- dermatitis from an exposure.

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