PPT 301 Pharmacology Week 12 Book Notes Chapters 34-36
PPT 301 Pharmacology Week 12 Book Notes Chapters 34-36 PPT 301
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This 9 page Class Notes was uploaded by Lexie Stenson on Friday April 8, 2016. The Class Notes belongs to PPT 301 at University of North Dakota taught by James Haselton in Spring 2016. Since its upload, it has received 30 views. For similar materials see Human physiology in Physiology at University of North Dakota.
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Date Created: 04/08/16
Pharmacology Week 12 Chapter 34 • Penicillin G o Therapeutic Class: Antibacterial o Pharmacologic Class: Cell wall inhibitor; natural penicillin o Actions and Uses: § Drug of choice against streptococci, pneumococci, and staphylococci organisms that do not produce penicillinase and are shown to be susceptible by C&S testing § Drug of choice for gonorrhea and syphilis § Available as either potassium or sodium salt; there isn’t a difference therapeutically between the two salts § Only 15-‐30% of an oral done of penicillin G is absorbed. Because of this low absorption, it is often given intravenously o Administration Alerts § After parenteral administration be sure to observe for possible allergic reactions for at least 30 minutes, especially after the first d § Do not mix penicillin and aminoglycosides in the same IV solution, give IV meds at least one hour apart o Adverse Effects § Diarrhea, nausea, and vomiting are the most common § Pain at injection site, superinfections are possible § Anaphylaxis is the most serious adverse effect § Contraindications • Hypersensitivity to the drug – because penicillin G is excreted by the kidneys, the drug should be used with caution in patients with severe renal disease o Interactions § Drug-‐Drug: Penicillin G may decrease the effectiveness of oral contraceptives. Colestipol taken with this drug will decrease absorption of penicillin. Potassium-‐sparing diuretics may cause hyperkalemia when administered with penicillin G potassium • Tetracycline o Therapeutic Class: Antibacterial o Pharmacologic Class: Tetracycline; protein synthesis inhibitor o Actions and Uses § Affective against a broad spectrum of gram-‐positive and gram-‐negative organisms including Chlamydia, Rickettsiae, and Mycoplasma. Use has increased over the last decade due to its effectiveness against H. Pylori in the treatment of peptic ulcer disease. Given orally, but has a short half life that may require a patient to take it up to fourt imes per day. Topical and oral preps are available for treating acne. Injections may cause local irritation and be very painful. o Administration Alerts § Give oral drug with full glass of water to decrease esophageal and GI irritation § Administer antihyperlipidemic and tetracycline 1 to 3 hours apar t o Adverse Effects § Tendency to affect vaginal, oral, and intestinal flora and cause superinfections. Irritates the GI mucosa and may cause nausea, vomiting, epigastric burning, and diarrhea. § Contraindications • Drug should not be used during the second half of pregnancy, in children 8 years or younger, or in patients with severe renal or hepatic impairment o Interactions § Drug-‐Drug: Milk products, iron supplements, magnesium-‐containing laxatives, and antacids reduce the absorption and serum levels of tetracyclines • Tetracyclines bind with the lipid-‐lowering drugs colestipol and cholestyramine, thereby decreasing the antibiotic’s absorption. • Also lowers the effectiveness of oral contraceptives • Erythromycin o Therapeutic Class: Antibacterial o Pharmacologic Class: Macrolide; protein synthesis inhibitor o Actions and Uses § Inactivated by stomach acid and is thus formulated as coated, acid-‐ resistant tablets or capsules that dissolve in the small intestin § Main application is for patients who don’t tolerate penicillins or who may have a penicillin-‐resistant infection § Effective against for gram-‐positive bacteria § Preferred drug against Bordetella pertussis (whooping cough), Legionella pneumophila (Legionnaire’s disease), M. pneumoniae, and Corynebacterium diptheriae o Administration Alerts § Administer on an empty stomach with full glass of water § Do not give with or immediately before or after fruit juices o Adverse Effects § Most frequent are nausea, abdominal cramping, and vomiting, although these are rarely serious enough to cause discontinuation of therapy § Hearing loss, vertigo, and dizziness may be experienced when on high doses, particularly in older adults and in those with impaired hepatic or renal excretion o Interactions § Drug-‐Drug: Anesthetics, azole antifungals, and anticonvulsants may interact to cause serum drug levels of erythromycin to rise and result in toxicity • Gentamicin o Therapeutic Class: Antibacterial o Pharmacologic Class: Aminoglycoside; protein synthesis inhibitor o Actions and Uses § Usually prescribed for serious urinary, respiratory, nervous, or GI infections when less toxic antibiotics are contraindicated § Effective against few gram-‐positive bacteria including some strains of MRSA § Often used on combination with other antibiotics such as penicillins or cephalosporins § Not absorbed by the oral route, a topical formula is available for infections of the external eye o Administration Alerts § For IM administration, give deep into large muscle § Use only IM and IV solutions that are clear and colorless or slightly yellow. Discard discolored solutions or those that contain particulate matter o Adverse Effects § Rash, nausea, vomiting, and fatigue are the most common § Resistance to Gentamicin is increasing, and some cross resistance among aminoglycosides has been reported § Black Box Warnings • Adverse effects from parenteral gentamicin may be severe and include the following: o Neurotoxicity o Neuromuscular blockade and respiratory paralysis are possible o Nephrotoxicity is possible o Interactions § Drug-‐Drug: risk of ototoxicity increases if patient is currently taking amphotericin B, furosemide, aspirin, bumetanide, ethacrynic acid, cisplatin, or paromomycin • Ciprofloxacin o Therapeutic Class: Antibacterial o Pharmacologic Class: Fluoroquinolone; bacterial DNA synthesis inhibitor o Actions and Uses § Most widely prescribed drug in its class. y inhibiting bacterial DNA gyrase, it affects bacterial replication and DNA repair § More effective against gram-‐negative that gram-‐positive organisms. Prescribed for UTI, sinusitis, pneumonia, skin, bone, and joint infections, infectious diarrhea, and serious eye infections o Administration Alerts § Administer at least 4 hours before antacids and ferrous sulfates o Adverse Effects § Serious adverse effects are uncommon § Nausea, vomiting, and diarrhea may occur in as many as 20% of patients, some patients report phototoxicity, headache, and dizziness § Black Box Warning • Tendinitis and tendon rupture may occur in patients of all ages. Risk is especially high in patients older that 60; in kidney, heart, and lung transplant recipients; and in those receiving concurrent corticosteroid therapy o Interactions § Drug-‐Drug: Concurrent administration with warfarin may increase anticoagulant effects and result in bleeding • Trimethoprim-‐Sulfamethoxazole o Therapeutic Class: Antibacterial o Pharmacologic Class: Sulfonamide; folic acid inhibitor o Actions and Uses § Most commonly prescribed for UTIs (aka Bactrim) § Also approved for treatment of Pneumocystis carinii Pneumonia, shigella infections of the small bowel, and for acute episodes ofc hronic bronchitis. Oral and IV preps are available § Inhibitors of the bacterial metabolism of folic acid o Administration Alerts § Administer oral doses with a full glass of water o Adverse Effects § Nausea and vomiting are the most common § Hypersensitivity in the form of skin rash, itching, and fever § Should be used with caution in patients with preexisting kidney disease, because crystalluria, oliguria, and renal failure have been reported. § Photosensitivity is often reported so patient should avoid direct sunlight during therapy o Interactions § Drug-‐Drug: May enhance the effects of oral anticoagulants • Isoniazid o Therapeutic Class: Antituberculosis drug o Pharmacologic Class: Mycolic acid inhibitor o Actions and Uses § First-‐line drug for the treatment of M. tuberculosis because decades of experience have shown it to have a superior safety profile and to be the most effective, single drug for the infection § Acts by inhibiting the synthesis of mycolic acids § It is bacteriocidal for actively growing organisms but bacteriostatic for dormant mycobacteria § It is selective for M. tuberculosis o Administration Alerts § Give on an empty stomach 1 hour after or 2 hours before meals o Adverse Effects § Numbness of hands and feet, rash, and fever. Neurotoxicity is a concern during therapy—patients may exhibit paresthesia of the feet and hands, convulsions, optic neuritis, dizziness, coma, memory loss, and various psychoses § Black Box Warnings • Hepatotoxicity is a serious and sometimes fatal adverse effect. However, very rare o Interactions § Drug-‐Drug: Aluminum-‐containing antacids should not be administered concurrently because they can decrease the absorption of the drug • Amphotericin B o Therapeutic Class: Antifungal (systemic type) o Pharmacologic Class: Polyene o Actions and Uses § Effective against most of the fungi pathogenic to humans; thus it is a preferred drug for many systemic mycoses § Prophylactic antifungal therapy for patients with severe immunosuppression § Not absorbed in the GI tract and is often given through IV infusion o Administration Alerts § Infuse slowly because cardiovascular collapse may result if medication is infused too rapidly § Administer premedication, such as acetaminophen, antihistamines, and corticosteroids, to decrease the risk of hypersensitivity reactions o Adverse Effects § Adverse effects of this drug can be frequent and serious including fever and chills, vomiting, and headache at the beginning of therapy o Interactions § Drug-‐Drug: Amphotericin B reacts with many drugs • Fluconazole o Therapeutic Class: Antifungal o Pharmacologic Class: Inhibitor of fungal cell membrane synthesis; azole o Actions and Uses § Acts by interfering with the synthesis of ergosterol, however offers several advantages over other systemic antifungals. It is rapidly and completely absorbed with given orally, and is particularly effective against Candida albicans § Major disadvantage of this drug is its narrow spectrum of activity o Administration Alerts § Do not mix IV with other drugs o Adverse Effects § Well-‐tolerated by most patients. § Nausea, vomiting, and diarrhea are reported at high doses § Hepatoxicity is rare with this drug o Interactions § Drug-‐Drug: Strong inhibitor of hepatic CYP enzymes and has the potential to interact with many drugs • Nystatin o Therapeutic Class: Superficial antifungal o Pharmacologic Class: Polyene o Actions and Uses § Binds to sterols in the fungal cell membrane, causing leakage of intracellular contents as the membrane becomes weakened § Available in a cream, ointment, powder, tablet, and lozenge § Too toxic for parenteral administration, primarily used topically for candida infections of the vagina, skin, and mouth § Is not absorbed in the GI tract o Administration Alerts § Apply with swab to the affected area in infants and children because swishing is difficult or impossible § For oral candidiasis the drug should be swished in the mouth for at least 2 minutes o Adverse Effects § Topically, produces few adverse effects other that minor skin irritation § High incidence of contact dermatitis § When given PO it may cause diarrhea, nausea, and vomiting o Interactions § Drug-‐Drug: unknown • Chloroquine o Therapeutic Class: Antimalarial drug o Pharmacologic Class: Heme-‐complexing agent o Action and Uses § Developed to count the high incidence of malaria § Is effective in treating the erthrocytic stage but has no effect on the latent Plasmodium § Concentrates in the food vacuoles of Plasmodium residing in red blood cells. Once in the vacuoles it is thought to prevent the metabolism of heme, which then builds to toxic levels within the parasite § Can reduce the high fever of patients in the acute stage in less than 48 hours § Also used to prevent malaria by being administered 2 weeks before patient enters into endemic area and continuing 4-‐6 weeks after the patient leaves o Administration Alerts § Pediatric dosage should be monitored closely § IM should be injected into a deep muscle and aspirate prior to injecting the medication because of its irritating effects to the tissues o Adverse Effects § Few serious adverse effects at low to moderate doses § Nausea and diarrhea may occur § At higher doses, CNS and cardiovascular toxicity may be observed – symptoms include confusion, convulsions, reduced reflexes, hypotension, and dysrhythmias o Interactions § Drug-‐Drug: antacids and laxatives containing aluminum and magnesium can decrease chloroquine absorption and must not be given within 4 hours of each other. May also interfere with rabies vaccine • Metronidazole o Therapeutic Class: Anti-‐infective, antiprotozoan o Pharmacologic Class: Drug that disrupts nucleic acid synthesis o Actions and Uses § Affective against both the intestinal and hepatic stages of the amebiasis § Preferred therapy for giardiasis and trichomoniasis § Antibiotic activity against anaerobic bacteria and thus is used to treat a number of respiratory, bone, skin, and CNS infections o Administration Alerts § Extended-‐release form must be swallowed whole and taken on an empty stomach § Contraindicated during first trimester of pregnancy o Adverse Effects § Anorexia, nausea, diarrhea, dizziness, and headache. § Black box warning • Drug is a carcinogen in lab animals and should be used only for approved indications o Interactions § Drug-‐Drug: interacts with oral anticoagulants to potentiate hypoprothrombinemia • Mebendazole o Therapeutic Class: Drug for worm infections o Pharmacologic Class: Anthelminthic o Actions and Uses § Most widely prescribed anthelminthic in the U.S. § Used to treat a variety of infections including roundworm and pinworm. § It is a broad spectrum drug so it is useful in mixed helminth infection s § Effective against both adult and larval stages of said parasites § Very little of the drug is absorbed systemically so most remains int he intestines where it kills the pathogens o Administration Alerts § Drug is most effective when chewed and eaten with a fatty meal o Adverse Effects § Does not generally cause serious systemic side effects. § As the worms die, some abdominal pain, distension, and diarrhea may occur o Interactions § Drug-‐Drug: Carbamazepine and phenytoin can increase the metabolism of the drug • Zidovudine o Therapeutic Class: Antiretroviral o Pharmacologic Class: Nucleoside reverse transcriptase inhibitor (NRTI) o Actions and Uses § As the reverse transcriptase enzyme thymidine begins to synthesize viral DNA, it mistakenly uses zidovudine as one of the nucleosides, thus creating a defective DNA strand § Used in combination with other antiretrovirals for symptomatic and asymptomatic patients whoa re infected with HIV as well as for postexposure prophylaxis in health care workers who have been exposed to HIV § Resistant HIV strands are common o Administration Alerts § Administer on an empty stomach, with water only § Avoid administering with fruit juice o Adverse Effects § Fatigue, generalized weakness, anorexia, headaches, nausea, and diarrhea § Black Box warning • Rare cases of fatal lactic acidosis with hepatomegaly and steatosis o Interactions § Drug-‐Drug: Interacts with many drugs. • Efavirenz o Therapeutic Class: Antiretroviral o Pharmacologic Class: Nonnucleoside reverse transcriptase inhibitor (NNRTI) o Actions and Uses § Given PO in combination with other antiretrovirals in the treatment of HIV infection § Drug acts by inhibiting reverse transcriptase § Has the advantage of one-‐daily dosing and penetration into cerebrospinal fluid § Preferred drug for the initial therapy of HIV infection o Administration Alerts § Administer on an empty stomach § Administer at bed time to limit adverse CNS effects o Adverse Effects § Sleeping disorders, nightmares, dizziness, reduced ability to concentrate, and delusions § Symptoms gradually go away after 3-‐4 weeks of therapy § Rash is common and should be monitored o Interactions § Drug-‐Drug: Patients who are receiving antiepileptic medications metabolized by the liver may require periodic monitoring of plasma levels because efavirenz may increase the incidence of seizures • Lopinavir with Ritonavir o Therapeutic Class: Antiretroviral o Pharmacologic Class: Protease inhibitor o Actions and Uses § Lopinavir is the active component of the combination § The small amount of ritonavir inhibits the hepatic breakdown of lopinavir, thus permitting serum levels of lopinavir to increase by more than 100 -‐ fold o Administration Alerts § The oral solution form should be taken with food to enhance absorption; tablets may be taken with or without food o Adverse Effects § Most frequent problem reported is diarrhea § Head ache and GI related effects are common including nausea, vomiting, dyspepsia, and abdominal pain o Interactions § Drug-‐Drug: Lopinavir is extensively metabolized by hepatic enzymes, and drugs that undergo hepatic metabolism may interact with this drug • Acyclovir o Therapeutic Class: Antiviral for herpesviruses o Pharmacologic Class: Nucleoside analog o Actions and Uses § Drug of choice for treatment of herpesviruses § Most effective against HSV-‐1 and HSV-‐2, and is effective only at high doses against CMV and varicella zoster § Prevents viral DNA synthesis o Administration Alerts § When given IV, the drug may cause painful inflammation of vessels at the site of infusion § Administer around the clock § Administer with food o Adverse Effects § Few adverse effects when given topically or orally § Nephrotoxicity and neurotoxicity are possible when medication is given IV o Interactions § Drug-‐Drug: concurrent use of acyclovir with nephrotoxic agents should be avoided
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