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Salicylic acid has a half-life of 2 to Other drugs related to this group are etodolac (Lodine) quetiapine 50mg mastercard, 3 hours at low doses and 6 to 12 hours at therapeutic anti- ketorolac (Toradol) quetiapine 50mg otc, and nabumetone (Relafen). It undergoes oxidation and conjugation portedly causes less gastric irritation, especially in older in the liver and its metabolites are excreted through the kidneys. Ketorolac is used only for In alkaline urine (eg, pH of 8), renal excretion of salicylate is pain, and although it can be given orally, its unique charac- greatly increased. Parenteral ketoro- Aspirin is a home remedy for headaches, colds, inﬂuenza lac reportedly compares with morphine and other opioids in and other respiratory infections, muscular aches, and fever. How- can be purchased in plain, chewable, enteric-coated, and ef- ever, its use is limited to 5 days because it increases the risk fervescent tablets and rectal suppositories. Hematomas and wound bleeding have been re- in liquid form because it is unstable in solution. Diﬂunisal (Dolobid) is a salicylic acid derivative that dif- Oxicam drugs include meloxicam (Mobic) and piroxicam fers chemically from aspirin. Meloxicam has a serum half-life of 15 to 20 hours rior to aspirin in mild to moderate pain, rheumatoid arthritis, (text continues on page 108) CHAPTER 7 ANALGESIC–ANTIPYRETIC–ANTI-INFLAMMATORY AND RELATED DRUGS 105 Drugs at a Glance: Analgesic, Antipyretic, Anti-inﬂammatory Drugs Routes and Dosage Ranges Generic/Trade Name Indications for Use Adults Children Comments Acetaminophen Pain PO 325–650 mg q4–6h, PO 10 mg/kg or accord- Warning: Overdoses may (Tylenol, others) Fever or 1000 mg three or ing to age as follows: cause fatal liver dam- four times per day; 0–3 mo, 40 mg; age. Maximum recom- maximum 4 g/d 4–11 mo, 80 mg; mended dose for adults 1–2 y, 120 mg; 2–3 y, is 4 g/d, from all 160 mg; 4–5 y, 240 mg; sources. Parents and 6–8 y, 320 mg; 9–10 y, caregivers should ask 400 mg; 11 y, 480 mg. Rectal suppository 650 mg Rectal suppository: age q4–6h, maximum of under 3 y, consult 6 in 24 h physician; age 3–6 y, 120 mg q4–6h, maxi- mum, 720 mg in 24 h; age 6–12 y, 325 mg q4–6h, maximum 2. RA: PO 150–200 mg/d in two, three or four divided doses (continued) 106 SECTION 2 DRUGS AFFECTING THE CENTRAL NERVOUS SYSTEM Drugs at a Glance: Analgesic, Antipyretic, Anti-inﬂammatory Drugs (continued) Routes and Dosage Ranges Generic/Trade Name Indications for Use Adults Children Comments Ankylosing spondylitis AS: PO 100–125 mg/d in Diclofenac sodium is (AS) four or ﬁve divided available in 25-, 50-, Pain, dysmenorrhea doses (eg, 25 mg four and 75-mg delayed- or ﬁve times daily) release tablets and a Pain, dysmenorrhea: 100-mg extended- (diclofenac potassium release (XR) tablet. It only) PO 50 mg three is not recommended times daily for acute pain or dys- menorrhea.
Available immunosuppressants inhibit the immune response by blocking that response at various sites discount quetiapine 100 mg without a prescription. Thus purchase 200 mg quetiapine mastercard, in rheumatoid arthritis, the antigen sue and organ transplantation, and rejection reactions are is a protein found in joint tissue. The mechanisms by which autoantigens are altered to elicit an immune response are unclear. Once tem loses its ability to differentiate between antigens on its an autoantigen is changed and perceived as foreign or non- own cells (called self-antigens or autoantigens) and antigens self, the immune response may involve T lymphocytes in on foreign cells. As a result, an undesirable immune response direct destruction of tissue, production of proinﬂammatory is aroused against host tissues. In most instances, the auto- cytokines that recruit and activate phagocytes, and stimulation CHAPTER 45 IMMUNOSUPPRESSANTS 673 Drugs at a Glance: Immunosuppressants Generic/Trade Name Indications for Use Contraindications Routes and Dosage Ranges Azathioprine (Imuran) Prevent renal transplant rejection Pregnancy Renal transplant: PO, IV Severe rheumatoid arthritis un- Allergy to azathioprine 3–5 mg/kg/d initially, de- responsive to other treatment creased (1–3 mg/kg/d) for maintenance and in presence of renal impairment Rheumatoid arthritis: PO 1 mg/kg/d (50–100 mg), in- creased by 0. Basiliximab (Simulect) Prevent renal transplant rejection Hypersensitivity to any components Adults: IV 20 mg within 2 h before of the drug formulation transplantation and 20 mg 4 d after transplantation (total of two doses) Children (2–15 y): IV 12 mg/m2 up to a maximum of 20 mg for two doses as for adults Cyclosporine Prevent rejection of solid organ Allergy to cyclosporine or poly- Sandimmune, PO 15 mg/kg 4–12 h (Sandimmune, Neoral) (eg, heart, kidney, liver) trans- oxyethylated castor oil (in IV before transplant surgery, then plant preparation only) 15 mg/kg once daily for 1–2 wk, Prevent and treat graft-versus-host Cautious use during pregnancy or then decrease by 5% per week disease in bone marrow trans- lactation to a maintenance dose of plantation 5–10 mg/kg/d Neoral, PO, the ﬁrst dose in clients with new transplants is the same as the ﬁrst oral dose of Sandimmune; later doses are titrated according to the desired cyclosporine blood level IV 5–6 mg/kg infused over 2–6 h Daclizumab (Zenapax) Prevent renal transplant rejection Hypersensitivity to any compo- IV 1 mg/kg over 15 min. First dose nents of the drug formulation within 24 h before transplanta- tion, then a dose every 14 d for four doses (total of ﬁve doses) Etanercept (Enbrel) Rheumatoid arthritis Sepsis Adults: SC 25 mg twice weekly, Hypersensitivity to any compo- 72–96 h apart nents of the drug formulation Children (4–17 y): SC 0. Tacrolimus (Prograf) Prevent liver, kidney, and heart Hypersensitivity to the drug or Adults: IV infusion, transplant rejection the castor oil used in the IV 25–50 mcg/kg/d, starting no formulation sooner than 6 h after transplan- tation, until the patient can tolerate oral administration, usually 2–3 d PO 150–200 mcg/kg/d, in two di- vided doses q12h, with the ﬁrst dose 8–12 h after stopping the IV infusion Children: IV 50–100 mcg/kg/d PO 200–300 mcg/kg/d of B lymphocytes to produce autoantibodies that produce develops serious infections and other adverse effects because inﬂammation and tissue damage. Serious com- One of these factors may be a deﬁcient number of suppressor plications can occur. At present, it is unclear whether suppressor T cells are a separate group or a subpopulation of helper or cytotoxic T cells with suppressive functions. The immune Tissue and organ transplantation usually involves replacing cells of the transplant recipient attach to the donor cells of the diseased host tissue with healthy donor tissue. Skin and renal grafts are commonly and successfully per- antibodies, multiple cytokines, and inﬂammatory mediators. In formed; heart, liver, lung, pancreas, and bone marrow trans- general, T cell activation and proliferation are more important plantations are increasing.
This reuptake can be inhibited by cocaine and tri- tagonistic action include sweating and regulation of arteriolar cyclic antidepressant medications and is responsible for the blood vessel diameter generic quetiapine 300 mg online, which is controlled by the SNS discount quetiapine 300 mg online. The remainder of the norepinephrine, which was not receptors are collectively called ligands. When receptors lo- taken back into the nerve endings, diffuses into surrounding cated on target tissues are stimulated by a ligand, a cascade tissue ﬂuids and blood, or it is metabolized by monoamine of intracellular events known as signal transduction is initi- oxidase (MAO) or catechol-O-methyltransferase (COMT). The ligand that binds the receptor is the so-called ﬁrst Norepinephrine also functions as a hormone, along with messenger. In response to adrenergic nerve stimulation, nor- tivates a cell membrane-bound G protein and an effector en- epinephrine and epinephrine are secreted into the bloodstream zyme that then activate a molecule inside the cell called a by the adrenal medullae and transported to all body tissues. This second messenger is the link be- They are continually present in arterial blood in amounts that tween events that are occurring outside the cell (ie, receptor vary according to the degree of stress present and the ability activation by the ligand) and resulting events that will occur of the adrenal medullae to respond to stimuli. The larger pro- inside the cell, such as opening ion channels, stimulating portion of the circulating hormones (approximately 80%) is other enzymes, and increasing intracellular calcium levels. These catecholamines exert the same effects as These intracellular events ultimately produce the physiologic those caused by direct stimulation of the SNS. However, the responses to neurotransmitter and hormone release or drug effects last longer because the hormones are removed from the administration. These hormones are metabolized mainly of signal transduction that occur when an adrenergic beta re- in the liver by the enzymes MAO and COMT. The SNS is stimulated by physical or emotional stress, such Adrenergic Receptors as strenuous exercise or work, pain, hemorrhage, intense emotions, and temperature extremes. Increased capacity for When norepinephrine and epinephrine act on body cells that vigorous muscle activity in response to a perceived threat, respond to sympathetic nerve or catecholamine stimulation, whether real or imaginary, is often called the ﬁght-or-ﬂight they interact with two distinct adrenergic receptors, alpha and reaction. Increased arterial blood pressure and cardiac output nephrine acts on both alpha and beta receptors. Increased blood ﬂow to the brain, heart, and skeletal tors have been further subdivided into alpha1, alpha2, beta1, muscles; decreased blood ﬂow to viscera, skin, and and beta2 receptors. A beta3 receptor has been identiﬁed, and other organs not needed for ﬁght-or-ﬂight animal studies suggest that drugs targeted to this receptor 3. Increased rate of cellular metabolism—increased oxy- may augment heat production, produce lipolysis (thermoge- gen consumption and carbon dioxide production nesis), and increase energy expenditure.
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