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Antibacterial drugs may work in one of four ways:


1. Interference with bacterial cell wall synthesis (penicillin);


2. Increase the permeability of the bacterial cell membrane, allowing leakage of the bacterial cell contents (polymixin);


3. Interference with protein synthesis and reproduction (tetracycline);


4. Interference with the synthesis of essential metabolites (sulfonamides).

Antiviral agents decrease the reproduction of viruses inside the host cell but cannot destroy the virus. They control, but do not cure infections.

Antifungal agents may interfere with the mitosis in fungi, or they may increase fungal membrane permeability. Most antifungal agents administered topically to skin or mucous membranes.

Treatment of Infection


- Complicated by the great variety of medications available and their differing modes of action


- First step: identify the causative organism and specific medication to which it is sensitive


= Culture and sensitivity (C&S) tests


- (eg. wound, throat, urine or blood) based on symptoms (results will not be available for 24-49 hours)


- physician may order an empiric (best guess based on history) anti-infective regimen that would likely be active against organisms encountered at given site.

Resistance


- Organisms may build up resistance to drugs and are therefore, no longer effective because of:


= Frequent use


= Incomplete treatment


Anti-infective resistance is caused by many factors


- Complex strategies needed to combat the problem

Selection of anti-infective drugs Infection site


- Status of hepatic and/or renal function


- Patient age


- Pregnancy or lactation (can damage developing fetus) (tetracycline or streptomycin)- breastmilk


- Likelihood of organisms developing resistance


- Known allergy to the anti-infective drug

Adverse Reactions


Categories


- Allergic hypersensitivity


= Over-response of the body to a specific substance


- mild reaction (rash, urticaria (hives) or mild fever) usually treated with corticosteroids or antihistamines


- Severe reactions manifested as anaphylaxis (sudden onset of dyspnea, chest constriction, shock and collapse) - unless treated promptly with epinephrine, corticosteroids, and CPR, death may result


- Direct toxicity


= Results in tissue damage (ototoxicity), nephrotoxicity, hepatotoxicity, blood dyscrasias, phlebitis, or phototoxicity


- Indirect toxicity or superinfection


= Manifested as a new infection due to absence of normal flora in the intestines or mucous membranes (esp with broad-spectrum antibiotics, allow colonization of different resistant bacteria or fungi)


- Treatment: antifungal meds, (buttermilk or yogurt in diet) administer probiotics, help restore normal intestinal flora


- Symptoms of Superinfections (diarrhea, vaginitis, stomatitis, or glossitis)

Vaccines/ Immuniziations


Centers for Disease Control and Prevention (CDC)


- Currently recommends routine vaccination


= Prevent 17 vaccine-preventable diseases that occur in infants, children, adolescents, or adults


= Information regarding vaccines and immunizations changes from time to time and requirements may vary by state, territory, or country

Aminoglycosides


Ex: gentamicin


Treats many infections caused by:


- Gram-negative bacteria (e.g., Escherichia coli and Pseudomonas)


- Gram-positive bacteria (e.g., Staphylococcus aureus)


- Enterococci may be resistant to aminoglycosides


Effective in short-term treatment of many serious infections


= Septicemia (e.g., bacteria in bloodstream causing low blood pressure) when less toxic drugs are ineffective or contraindicated


Ex: of Aminoglycosides: amikacin, gentamicin and tobramycin)


- poor absorption from GI tract, usually administered parenterally (ie. IM or IV)


- Serum levels peak and trough - determine optimal dosing and lessen risk of side effects.


Serious Side Effects: esp in older adults, dehydrated patients or those with renal or hearing impairment


= nephrotoxicity, Otoxicity, Neuromuscular blockade (respiratory paralysis), CNS symptoms (headache, tremor, lethargy, numbness, and seizures), blurred vision, rash or urticaria.

Cephalosporin


Semisynthetic beta-lactam antibiotic derivatives produced by a fungus


- Related to penicillins


= Some patients allergic to penicillin are also allergic to cephalosporins


- Classified as first, second, third, or fourth, or fifth generation


= According to organisms susceptible to their activity


- active against gram-positive and gram-negative bacteria


5 gen: cephalexin effective against gram + and some gram - organisms(skin soft tissue UTI)


2 gen: cefaclor effective against many gram+ and gram- organisms (cause bacterial pneumonia)


3 gen: ceftriaxone effective against more gram- bacteria sometimes used to treat STIs (gonorrhea)


- Ceftazidime extremely active against Pseudomonas aeruginosa.


4 gen: Cefepime (Maxipime) parenteral cephalosporin with excellent activity against gram + and gram -



Macrolides


- Treats many infections of the respiratory tract, skin conditions, or for some sexually transmitted infections


- Considered among the least toxic antibiotics Preferred for treating susceptible organisms under conditions in which more toxic antibiotics might be dangerous

Penicillin


Beta-lactam antibiotics produced from certain species of a fungus


- Treats many streptococcal and some staphylococcal and meningococcal infections


- Drug of choice for treatment of syphilis


- Used prophylactically to prevent recurrences of rheumatic fever


- Amoxicillin preferred for infective endocarditiis prophylaxis in dental procedures ( 2g orally 1 h prior to procedure) used with combo with drugs to treat H. pylori infection with duodenal ulcer disease

Carbapenems


Belong to the beta-lactam class of antibiotics


- Have a very broad spectrum of activity against gram-negative and gram-positive organisms


- Primary treatments include pneumonia, febrile neutropenia, intra-abdominal infections, diabetic foot infections, and significant polymicrobial infections

Quinolones


For adult treatment of some infections of the urinary tract, sinuses, lower respiratory tract, GI tract, skin, bones, and joints, and in treating gonorrhea


- Some organisms are showing increased resistance


- Reserve for infections that require therapy with a fluoroquinolone

Tetracycline


Broad-spectrum antibiotics


- Treats infections caused by rickettsia, chlamydia, or some uncommon bacteria


- Some organisms are showing increasing resistance


- Use only when other antibiotics are ineffective or contraindicated

Anti-fungals


Treat specific susceptible fungal disease


- Medications are quite different in action and purpose


Amphotericin B


- Administered IV for the treatment of severe systemic and potentially fatal infections caused by susceptible fungi, including Candida


Fluconazole


- Works against many fungal pathogens, including most Candida, without the serious toxicity of amphotericin B


Micafungin (Mycamine)


- Given IV


- Provides new treatment options against Candida and Aspergillus species


Nystatin


- Structurally related to Amphotericin B


- Orally treats oral cavity candidiasis


- Also used as a fungicide in the topical treatment of skin and mucous membranes

Antituberculosis Agents


Tuberculosis (TB)


- Caused by a bacterium called Mycobacterium tuberculosis, which primarily attacks the lungs


Antituberculosis agents are administered for two purposes


- To treat latent or asymptomatic infection (no evidence of clinical disease)


- For treatment of active clinical tuberculosis and to prevent relapse



= treatment of TB is challenging for 2 reasons


1. increasing incidence of TB found particularly in high-risk pop


2. Organisms have become resistant (multidrug and extensive drug resistant) due to patient noncompliance or failure to complete 6-24 month conventional treatment)



Miscellaneous Anti-infectives


Clindamycin


- Treats serious respiratory tract infections, septicemia, osteomyelitis, serious infections of the female pelvis caused by susceptible bacteria, and for Pneumocystis jirovecii pneumonia associated with AIDS


- Prophylactic use in dental procedures for penicillin-allergic patients


- May be a viable therapeutic option for community-acquired MRSA (Methicillin-resistant Staphylococcus aureus)

Miscellaneous Anti-Infectives


Metronidazole (Flagyl)


- Synthetic antibacterial and antiprotozoal agent


- Effective against protozoa


- One of the most effective drugs against anaerobic bacterial infections


- Also useful in treating Crohn’s disease, antibiotic-associated diarrhea, rosacea, and


H. pylori infection


Vancomycin


- Structurally unrelated to other available antibiotics (effective against MRSA)


- IV vancomycin is used in the treatment of potentially life-threatening infections caused by susceptible organisms

Agents for VRE


Linezolid (Zyvox)


- Indicated for gram-positive infections


- Approved for the treatment of bacterial pneumonia skin, skin structure infections, and MRSA and VRE infections


- Effective in treating diabetic foot infections


- Administered by IV infusion or orally

Sulfonamides


Among the oldest anti-infectives


- Increasing resistance of many bacteria has decreased the clinical usefulness of these agents


Used most effectively in combinations with other drugs


- Example: Trimethoprim: sulfamethoxazole and trimethoprim (Bactrim) (used to treat UTIs)


- Resistance develops more slowly

Urinary Anti-Infectives


Urinary tract infection (UTI)


- Symptomatic inflammatory response from the presence of microorganisms in the urinary tract


- One of the most common bacterial infections for which patients seek treatment


- First-line urinary anti-infectives for empiric treatment of uncomplicated lower UTI are sulfamethoxazole-trimethoprim and nitrofurantoin (take 5-7 days)

Anti Virals


Acyclovir


- Primarily treats herpes simplex, herpes zoster (shingles), and varicella zoster (chickenpox) infections


Neuraminidase inhibitors


- Indicated for the treatment of uncomplicated acute illness due to influenza types A and B


Ribavirin


- Treats infants and young children with respiratory syncytial virus (RSV) infections via nasal and oral inhalation

Treatment of HIV/AIDS Infections


Highly specialized field


- Those actively practicing in that field must be updated frequently on the many new medications and frequently changing protocols


Treatment of HIV infection


- Consists of using highly active antiretroviral therapy (HAART) combinations of three or more antiretroviral (ARV) agents

Treatment of HIV/AIDS Infections


Antiretroviral protease inhibitors (PIs)


- Block the activity of the HIV enzyme essential for viral replication late in the virus life cycle


Nucleoside reverse transcriptase inhibitors (NRTIs)


- Inhibit an enzyme responsible for viral replication early in the virus life cycle

Treatment of HIV/AIDS Infections


Non-nucleoside reverse transcriptase inhibitors (NNRTIs)


- Inhibit an enzyme responsible for viral replication early in the viral life cycle


Fusion inhibitors (FIs)


- Block entry of HIV into cells, which may keep the virus from reproducing

Treatment of HIV/AIDS infections


CCR5 antagonists


- Block a co-receptor required for HIV entry into human cells


Integrase inhibitor


- Raltegravir (Isentress): first ARV designed to slow the advancement of HIV infection by blocking the enzyme needed for viral replication

HIV Information and Resources


Sources of current recommendations for clinical use of antiretrovirals (ARVs)


- Department of Health and Human Services


- Florida/Caribbean Aids Education and Training Center


- AETC National Resource Center Drug Interactions


- Johns Hopkins HIV GuideNational HIV Telephone Consultation Service


- University of California, San Francisco

Chapter 18 Eye medications



Introduction:


Most common eye diseases in Americans 40 years and older


- Age-related macular degeneration, glaucoma, cataracts, and diabetic retinopathy


Conjunctivitis: inflammation of the conjunctiva - One of the most frequent causes of patient seeking help

Medications for Eye


Medications for the eye


- Anti-infectives


- Anti-inflammatory agents


- Antiglaucoma agents


- Mydriatics (pupil dilation)


- Local anesthetics

Anti-Infectives


Treat superficial eye infections caused by susceptible organisms


- Ointments are preferable to drops in children and patients with poor adherence


- Drops are preferred in adults


= Ointments will cause blurring of vision for 20 minutes after instillation


- Determine causative organism when possible

Anti-Inflammatory Agents


- Relieve eye or conjunctiva inflammation in allergic reactions, burns, postoperatively, or irritation from foreign substances


- Corticosteroids


= Useful in acute stages of eye injury


- Prevent scarring, for severe symptoms, or when condition is unresponsive to other medications


- Nonsteroidal anti-inflammatory drugs (NSAIDs)


= Treat postoperative inflammation following cataract surgery


= Alternative to corticosteroids if a contraindication exists

Anti-Inflammatory Agents


Antihistamines/decongestants


- Block histamine receptors in conjunctiva, relieving ocular pruritis associated allergic conjunctivitis


- Cause vasoconstriction of blood vessels, providing relief from minor eye irritation and redness


Ophthalmic lubricants


- Provide a barrier function at the level of the conjunctival mucosa


- Help to dilute and flush various allergens and inflammatory mediators that may be present on the ocular surface

Antiglaucoma Agents


What is glaucoma?


- A group of sight-threatening diseases of the eye in which there is increased intraocular pressure (IOP) due to obstruction of outflow of aqueous humor


= Causes deterioration of and damage to the optic nerve resulting in vision loss



Antiglaucoma Agents


Glaucoma types


- Acute (angle-closure) glaucoma


= Characterized by a sudden onset of pain, blurred vision, and a dilated pupil


= Considered a medical emergency


- Chronic (open-angle) glaucoma


= Much more common


= Often bilateral


- Develops slowly over a period of years with few symptoms except a gradual loss of peripheral vision and possibly blurred vision



Antiglaucoma Agents


Antiglaucoma drugs given to lower intraocular pressure


- Carbonic anhydrase inhibitors: reduce formation of hydrogen and bicarbonate ions


= Diuretic effect; reduces production of aqueous humor


- Miotics: cause pupil to contract


= Reduce intraocular pressure by increasing aqueous humor outflow

Antiglaucoma Agents


Beta-adrenergic blockers: used topically to lower intraocular pressure in open-angle glaucoma


= Decreased rate of aqueous humor production


Alpha agonists: decreases formation and increases outflow of aqueous humor


= Minimal effects on cardiovascular or pulmonary hemodynamics

Antiglaucoma Agents


Prostaglandin analogs: greatest reduction in IOP by increasing outflow of aqueous humor


- May be used concomitantly with other topical ophthalmic drugs to lower IOP

Mydriatics


- Topically dilates the pupil for ophthalmic examinations


= Example: atropine


- Also acts as a cycloplegic (paralyzes the muscles of accommodation)


- Drug of choice in eye examinations for children


- Often used for adults because of fast action and fast recovery time



Local Anesthetics


- Applied topically to the eye for minor surgical and diagnostic procedures, removal of foreign bodies, or painful injury


= Example: tetracaine (TetraVisc)

Vancomycin - resistant enterococci (VRE) cause infections such as bacteremia, endcarditis, or UTRs (can be difficult to treat)


- limited treatment options and mortality rates high


= Strains of Type A influenza are now resistant to oseltamivir (Tamiflu)


Candida resistant to fluconazole (growing problem)

Precautions or contraindications with Aminoglycosides


- Tinnitus, vertigo, high-frequency hearing loss


- reduced renal function


- dehydration


- pregnant or nursing women


- infants or older adults

Interactions of aminoglycosides may occur with


- other ototoxic drugs (emphotericin B, polymixin B, bacitracin and vancomycin)


- general anesthetics or neuromuscular blocking agents (succinylcholine, can cause respiratory symptoms of ototoxicity)

Patient Education on aminoglycosides


- extreme importance of close medical supervision during therapy


- careful observation of intake and urinary output


- prompt reporting of side effects (esp hearing loss)

Side Effects of cephalosporins


- hypersensitivity (rash, edema, or anaphylaxis- esp allergic to penicillin)


- blood dyscrasias (increased bleeding time or transient leukopenia), renal toxicity, mild hepatic dysfunction)


- nausea, vomiting and diarrhea


- phlebitis with IV administration and pain at site of IM injection


- respiratory distress, seizures

Precautions or contraindications with cephalosporins


- known allergies (esp penicillin (3-7% cross sensitivity, more with first gen cephalosporins)


- prolonged use: lead to superinfections or severe colitis (c. difficile)


Interactions


- increased effectiveness with probenecid


- Disulfiram-like reactions (flushing, tachycardia, shock) with alcohol ingestion and cefotetan

Patient education on cephalosporins


- possible allergic reactions


- avoidance of alcohol


- reporting any side effects


- take meds without regard to meals but with food if stomach upset occurs


- attention to signs of abnormal bleeding (check stools and urine for blood)

Macrolides


- erythromycin, clarithrymycin and azithromycin used to treat many infections of respiratory tract for skin conditions (acne or some STIs when patient allergic to penicillin)


- least toxic antibiotics, preferred for treating susceptible organisms (toxic antibiotics might be dangerous- patients with renal disease, pregnant women or infants)


- giant gram-neg bacilli generally resistant to macrolides and resistant to strains of Group A Streptococci and Streptococcus pneumoniae


- Clarithromycin in combo with amoxicillin and lansoprazole (prevpac Kit) used to treat Helicobacter pylori infection with duodenal ulcer disease


- Erythromycin in low doses stimulates gastric emptying = used in treatment of GI motility disorders

Side effects from macrolides of serious nature rare and mild side effects


- anorexia, nausea, vomiting, diarrhea, and cramps (take meds with food or use smaller frequent doses)


- superinfections


- serious side effects occur with some interactions

Precautions or contraindications with Macrolides


- liver dysfunction and GI disease


- electrolyte imbalances certain cardiovascular disease (can cause abnormal changes in electrical activity of heart that may lead to potentially fatal irregular heart rhythm)




Interactions (erythromycin and clarithrymycin less with azithromycin) may occur with potentiation of folowing drugs and possible toxicity


- carbamazepine (Tegretol) (ataxia, dizziness and drowsiness)


- Cyclosporine (immunosuppressant with kidney or liver transplants)


- Theophylline


- Benzodiazepines (potentiation of sedative effects)


- Warfarin (may prolong prothrombin time and bleeding)


- digioxin


- statin (lead to myopathy)

Warning with Macrolides


- can cause abnormal, potentially fatal, cardiac arrhthmias when combined with


- Ca2+ channel blockers (verapmil or diltiazem)


- Antiarrhythmic agents (stalol)


Azole antifungals - fluconazole (Diflucan)


- Quinolones

Patient Ed with Macrolides


- common GI side effects - take meds with FULL glass of water 1 h before or 2 h after meals unless stomach upset occurs


- not taking with other meds (see interactions)

Penicillin


- Serious side effects: hypersensitivity (rash to fatal anaphylaxis)


- Superinfections (esp with oral ampicillin_ and pseudomembraneous colitis (C. difficile)


- Nausea, vomiting and diarrhea


- blood dyscrasias (reversible with discontinuance of drug)


- renal and hepatic disorders (rare)


- CNS effects, ex: confusion, anxiety and seziures (esp with penicillin G)



Precautions or contraindications with Penicillin


- history of serious allergy to penicillins or other beta-lactams


- treatment includes discontinue of drug, immediate admin of appropriate meds (epinephrine and corticosteroids), maintain patent airway. admin of antihistamines with penicillin will not prevent hypersensitivity reaction


Interactions of penicllins


- potentiation with probenecid


- potentiation with anti-inflammatory drugs (methotrexate and salicylates) at same time


- antagonistic effect (delay absorption) of oral penicillins when given with antacids or with food


- antagonistic effect of some other anti infectives on penicillin


- Penicillin V or ampicillin may inhibit action of estrogen-containing oral contraceptives.

Patient Ed of Penicillins


- discontinue of med and immediate reporting of any hypersensitivity reactions (rash, swelling or difficulty breathing)


- take meds on time for ex on empty stomach, 1 hour before or 2 hour after meals with full glass or water


- possible decreased effectiveness of estrogen containing oral contraceptives

Carbapenems


- Generic: meropenem, Trade: Merrem


-

Quinolones side effects


- nausea, vomit, diarrhea, abdomin pain, colitis (es older adults)


- CNS effects: headache, dizziness, confusion, irritability, seziures and anxiety


- crystalluria (drinking liberal quantities of fluids)


- superinfection


- hypersensitivity reactions or rash (rare)


- phototoxicity (esp to sun can cause severe sunburn)


- possible cartilage or tendon damage

Precautions/contradindication of Quinolones


- older adults esp with GI disease or Arteriosclerosis


- children or adolescents (potential for cartilage damage)


- those doing strenuous exercise during several weeks after therapy (potential for tendon rupture)


- pregnancy and lactation


- seizure disorders


- cardiac disease ( may cause or contribute to arrhythmias)


INteractions;
- Theophylline (ciprofloxacin can potentiate serious or fatal CNS effects, cardiac arrest or respiratory failure)


- Probenicid (increase blood levels of Cipro)


- warfarin (incrased risk of bleeding)
- Antacids and other prep containing Fe, Mg, Zn, Ca (decrease absorption (do not give within 2h)


- Sucralfate ( Carafate) contains aluminum ions - decrease absorption

Patient Ed for Quinolones


- not take other meds without approval


- drinking liberal quantities of fluids


- restrict caffeine intake (see CNS effects)
- avoid excessive exposure to sun


- avoid strenuous exercise during several weeks after therapy (cartilage or tendon damage)


- report all side effects (rash or hypersensitivity)


- Geriatric patients follow preceding instructions (report GI effects or CNS effects)

Tetracyclines


- treat Rocky Mountain (spotted fever) atypical pneuonia, some STIs, and severe inflammatory acne.


- Doxycycline can treat skin and skin structure infections caused by community acquired MRSA)


- combined with bismuth salicylate and metronidazole (Helidac Therapy Kit) treat H.pylori infection associated with duodenal ulcer disease

Side effects of Tetracyclines


- nausea, vomiting, diarrhea (frequently dose related)


- superinfections (vaginitis and stomatitis)


- photosensitivity with exaggerated sunburn


- discolored teeth in fetus or young children


- retarded bone growth in fetus or young children


- hepatic or renal toxicity (rare)


Interactions


- decrease absorption with following antagonist


- antacids, calcium supplements or magnesium laxatives


- Iron prep and zinc


- antidiarrheal agents containing kaolin, pectin or bismuth


0 dairy products (doxycycline and minocycline not significantly affected)


- oral contraceptives (breakthru bleeding or pregnancy may occur)

Tigecycline (Tygacil) derived from minocycline (IV antibiotic approved to treated intra-abdominal and skin structure infection caused by several microorganisms including MRSA)


- significant activity against VRE 0 reserve for more serious and resistant infections to maintain full spectrum activity.

Patient Eduction for Tetracycline


- avoid sun


- avoid med: if preg ornursing child under 8


- admin pref on empty stomach with full glass of water, 1hour before or 2 hour after meals unless there is gastric distress


- avoid iron, calcium, magnesium, and antidiarrheal agents or dairy foods within 2 hour of taking tetracyclines


- not taking at bedtime to prevent irritation from esophageal reflux


- discard any expired drug (nephrotoxicity can result from taking outdated drug)

Antifungals


Amphotericin B Side Effects


- headache, chills, fever, hypotension and tachypnea, infusion-related reactions


- malaise, muscle and joint pain, weakness


- anorexia, nausea, vomiting and cramps


- nephrotoxicity (occurs in most patients)


- anemia


- hypokalemia and hypomagnesemia


- Lipid-base product (Abelcet) incrases tolerability of drug without compromising antifungal effects)

Fluconazole (diflucan) antifungal


side effects:


- moderate nausea, vomiting, abdominal pain and diarrhea


- rash


- hepatic abnormalities


- dizziness and headache

Precautions or contraindications of Fluconazole


- pregnant or nursing


- hepatic or renal disease


Interactions


- Warfarin (increased prothrombin time could cause hemorrhage)


- oral antidiabetic agents (hypoglycemia can result)


- Rifampin (can lead to clinical failure of fluconazole)


- Statins (except pravastatin, increased risk of myopathy)


- Benzodiazepines (increased CNS effects)

Micafungin (mycamine) newer class of antifungals given IV, new treatment against Candida, and Aspergillus species


- indicated for treatment of esophageal candidiasis and candidemia and for stem cell transplant prophylaxis


Side effects:


= headache, fever, nausea, vomiting, diarrhea, infusion reactions


- neutropenia, hypokalemia and hypomagnesemia

Precautions/Contraindications of Micafungin


- patients under 18


- pregnancy and breast-feeding


- Liver dysfunction


- renal Disease


- no major drug interaction with Mycamine

Nystatin


- structurally related to amphotericin B


- used orally to reat oral cavity candidiasis


- used as fungicide in topical treatment of skin and mucous membranes (diaper area, mouth, or vagina)


Side effects: rare but include nausea, vomting, and diarrhea with high doses


Caution: pregnant women or nursing, no significant drug interactions due to lack of absorption from gut

Antituberculosis Agents


- CDC recommends following treatment regimen


1. ATS and CDC recommend short-course regimens (ie. 6months) treat uncomplicated pulmonary TB in adults. suitable for children, Directly observed therapy (DOT) used for all regimens administered 2 or 3 times per week when possible to ensure compliance)


2. initial regimen should include INH given once daily for 2 months (in combo with rifampin, pyrazinamide and ethambutol) followed by isoniazid and rifampin given daily; twice weekl or 3 times per week for additional 4 months


- HIV + patients should receive induction therapy with 4 drugs by DOT, treatment may be extended to 9 months or longer in HIV infected patients. (sputum cultures from positive to negative)

Patient Ed on Antifungal


- taking meds for prolonged periods as prescribed even after symptoms


- report relapses promptly to physician

Side effects of Antituberculosis


INH and rifampin


- nausea, vomiting and diarrhea


- dizziness, blurred vision, headache and fatigue


- numbness and weakness of extremities


- hepatic toxicity (esp those over 35 years and children)


- body fluids colored red-orange with rifampin


- hypersensitivity reaction with flu-like symptoms (sometimes with rifampin)

Precautions/contra with INH and rifampin


- chronic liver disease or alcoholics


- imparied renal function


- children's doses of INH and rifampin should be limited to 10 and 15 mg/kg respectively to decrease likelihood of hepatic toxicity


Interactions:


- antagonism by oral hypoglycemics, corticosteroids, digitalis, anticoagulatns, and estrogen (serum levels of these drugs reduced when taking rifampin)


- decreased in serum concentration of antiretroviral protease inhibitors (PIs) may result in HIV treatment failure



Interactions with INH


- potentiation by phenytoin (Dilantin) incrased action when taken with isoniazid


- increase risk of hepatotoxxicity with rifampin (vs each agent alone)


- alcohol (incrase possibility of liver toxicity with both INH and rifampin)


- antacids (avoid 2 hour before and after INH)


Side Effects: of ethambutol


- optic neuritis (visual problems - reversible if discontinued early)


- dermatitis, pruritus, headache, malaise, fever, confusion, joint pain and GI symptoms and occasional peripheral neuritis

precautions or contraindications with ethambutol


- visual testing before and during therapy


- impaired renal function (reduce dose)
- diabetes (diabetic retinopathy)
- ocular defects


- children under 13 only children whose visual acuity can accurate be determined/monitored


- pregnancy- caution


- patients with gout (ethambutol can cause hyperuricemia)


S

Side Effects of Pyarzinamide can include


- hepatic toxicity


- gout (increased uric acid)


- hypersensitivity


- GI disturbances


Precautions contraindications


- people with history of gout


- diabetes


- severe hepatic disease or alcoholism


- children (potential toxicity)


pregnant or nursing women

Side effects of streptomycin (common to all amiinoglycosides)
- ototoxicity


- nephrotoxicity


- streptomycin is administered by deep IM injection alternating sites



Patient ed taking antituberculosis


0 taking riampin on empty stomach for max absorption or with food if nauseated


- taking prescribed meds for length required period of time even though asymptomatic


- report side effects


- important checks lab checks


- red-orange color or urine, feces, sputum, sweat and tears with rifampin


- not wearing contact lens during rifampin treatment


- interactions with other drugs (eg. birth control pills may be ineffective)


- avoid alcohol


- importance of visual testing periodically during ethambutol treatment

Miscellaneous Anti-Infectives


Clindamycin


- side effects: nausea, vomiting, diarrhea and colitis (discontinue if symptoms develop)


- rash, pruritus, fever, and oaccasionally anaphylaxis)


- local effects (minimize by deep IM or frequent IV catheter change)

Precautions or contraindications of clindamycin


- history of GI, hepatic, or renal disease


- older adults, children lactation (not recommended)



Anti-infective agents: quinolones, tetracyclines, antifungals and antituberculosis agents


pg 313

Metronidazole (flagyl) antibacterial and antiprotozoal agent effective against protozoa: Trichomonas vaginalis and treat amebiasis and giardiasis


Side effects: abdom pain, nausea, vomiting


- anorexia, metallic taste, xerostomia (dry mouth)


- headache, dizziness, ataxia (defective muscle coordination


- flushing, rash, and urticaria


- peripheral neuropathy (rare) and seizures


- dark urine (common but harmless)

Precautions NMetronidazole


- history of blood dyscrasias


- lactation


- children (except treat of amebiasis)


- CNS and hepatic diseases


- Avoid alcohol during 48 hour after treatment (disulfriam-like" reaction symptoms: flushing, nausea, vomiting thirst, chest pain, vertigo and hypotension_

Vancomycin - unrelated to other antibiotics


- IV treat potentially life-threatening infections


- poorly absorbed after oral admin, NOT USEd orally for widespread infections.


- can be given orally to treat GI infections (c.diff)


Side effects: ototoxicity or nephroticity with older impure formulations with IV use (discontinue with tinnitus may preced deafness)


- local effects (give only IV with care, can cause necrosis or thrombophlebitis)


- Rash (Red Man's Syndrome" anaphylaxis and vascular collapse (hypersensitivity reaction reported in 5-10% patients


- pseudomembranous colitis caused by C. difficile infection (rare)

Precautions or contraindication with vancomycin


- older adults, hearing impairment, renal impairment, pregnancy and lactation

Vancomycin has been "last line of defense" against staphylococcal infections, and certain streptococcal and enterococcal infections




Linezolid (Zyvox) indicated for gram positive infections approved treat for bacterial pneumonia, skin, and skin structure infections and MRSA and VRE infections (including by bacteremia), treat foot infections diabetic


- administered IV infusion or orally implication fo med


Side effects: nausea, headache, diarrhea (stop med)


- anemia, and thrombocytopenia


- lactic acidosis


- psuedomembranous colitis

Precautions of Linezolid


- blood dyscrasias


- cardiac disease and hypertension


- GI disease and hyperthyroidism


- pregancy and lactation


- infants


Interactions:


- beta-blockers (worsen bradycardia)


- Antidepressant (e.g. SSRI can cause serotonin syndrome)


- migraine medications (triptans)


- sympathomimetrics such as phenylephrine and pseudophedrine (hypertensive reaction)
- food or bev with high tyramine content



Daptomycin (Cubicin) first new class of antibiotics called lipopeptides spectrum of activity similar to vancomycin


- greater activity against certain gram-positive bacteria


- promise in treating VRE infections and endocarditiis


Side effects: constipation, nausea, injection-site reactions, and headache


- elevated levels of creatinine phosphokinase CPK, lead to myopathy (monitor CPK levels)




Precautions


- renal impairment


- pneumonia

Pg 317 Miscellaneous Anti-infectives and Agents for VRE


Clindamycin


metronidazole


vancomycin




VRE: daptomycin, linezolid

Patient ed for antibiotics


- never taking antibiotics for viral infections


- never take antibiotics left over from treatment of previous infection or ones that were prescribed for someone else


- allergies: inform doctor


- if pregnant or breastfeeding inform doc


- take all antibiotics with full glass of water on empty stomach at least 1 hour before meals or 2 hour after meals (unless otherwise directed)


- not taking meds with alcohol, antacid or fruit juice


- taking antibiotics at prescribed times maintain blood levels, if miss dose, do not double next dose (resume with next scheduled dose)


- taking entire prescription completely, not discontinuing when symptoms of infection disappear


- not taking any other meds, prescriptions or OTC drugs at same time as antibiotics without checking first with physician/pharm

Sulfonamides and Urinary Anti-infectives pg 320


Antivirals(herpes, influenza, RSV) page 323


Drugs for HIV/AIDS pg 327



Chapter 18 Eye meds


anti-infective pg 334


anti inflammatory corticosteroids pg 335


NSAIDS pg 336


antihistamine or decongest, ophthalmic lubricants, ophthalmic immunologic agent g 337


Table Anti-inflammatory Ophthalmic Drugs338


Antiglaucoma agents 339


Carbonic Anhydrase Inhibitors 340


Miotics, Direct-acting 341


Beta-Adrenergic Blockers 342


Alpha agonist pg 343


Prostaglandin Analogs pg 344


Antiglaucoma Agents pg 345


Mydriatics pg 345


local anesthetics pg 346


Mydriatics and local anesthetics for eye 347



ll

Emiliano is having a stem cell transplant in hopes of curing his leukemia. The doctors explain that he will be at high risk of infection and, as a result, they will treat him prophactically to prevent the infections. What antifungal are the doctors likely to use?


= micafungin

Mina has a younger brother who has an autism spectrum disorder and she is worried that her infant son may also be diagnosed with the same disorder. She has heard that vaccines may cause autism and asks you about this. What should you tell your friend?


= The Institute of Medicine has determined that evidence is insufficient to demonstrate a causal relationship between vaccines and autism.

Five-year-old Thomas has brain cancer and chemotherapy and radiation have left him severely immunocompromised. He has a life threatening fungal infection that has not responded to other agents. The doctor tells his parents about a medication that may be his last chance, but emphasizes that severe side effects are expected. Which antifungal has this profile?


= amphotericin B

Sulfonamides


- oldest anti-infectives


- Sulfamethoxazole and trimethoprim (Bactrim) = treat UTIs, esp acute, complicated UTIs; enteritis and otitis media.


= treat and prevent P.jirovecii pneumonia in HIV-infected patients


= prevention of toxoplasmosis in HIV-infected persons


- higher doses (oral alternative to vancomycin) when treating certain MRSA infections



Side Effects of Sulfonamides


(numerous and sometimes serious esp in AIDS patient)


- rash, pruritus, dermatitis, and photosensitivity


- nausea, vomiting, and diarrhea


- high fever, headache, stomatitis and conjunctivitis


- blood dyscrasias


- hepatic toxicity with jaundice


- renal damage with crystalluria and hematuria


- hypersensitivity reactions (can be fatal)

Precautions or Contraindications with sulfonamides


- impaired hepatic function


- impaired renal function or urinary obstruction


- blood dyscrasias


- severe allergies or asthrma


- pregnancy or lactation

Interactions with Sulfonamides


- potentiation of anticoagulants and oral antidiabetics


- antagonism of local anesthetics (e.g. procaine may inhibit the antibacterial action of sulfa)


- potentiation of phenytoin (Dilantin) E.g. increasing serum drug concentration)


- ACE inhibitors, potassium salts, potassium-sparing diuretics (Hyperkalemia)




Patient Education


- importance of drinking large amounts of fluid to prevent crystalluria (crystals in urine)


- discontinuance of sulfa at first sign of rash


- report any side effects to physician immediately


- avoid exposure to sunlight


- ingestion of sulfa with food (delay but does not reduce absorption of drug)

Urinary Anti-Infectives


- UTI - symptomatic inflammatory response from presence of microorganisms in urinary tract (most common bacterial infections for patients to seek treatment)


- First Line Urinary Anti-Infective for empiric treatment of uncomplicated lower UTI


= sulfamethoxazole-trimethoprim and nitrofurantoin


Nitrofurantoin (Macrobid and Macrodantin) most commonly used for initial or recurrent UTIs caused by susceptible organisms.


= recommended oral treatment option for cystitis (bladder infection) in women not men (tissue concentration generally lower) = inadequate treatment of occult prostatitis


*nitrofurantoin never used to treat pyelonephritis in men or women

Side Effects of Nitrofurantoin


- nausea and vomiting (less frequent if taken with milk or food)


- numbness and weakness of lower extremities


- headache, dizziness and weakness of muscles


- cough; respiratory distress with prolonged use


- dark yellow or brown-colored urine


- hemolytic anemia

Precautions or contraindications with nitrofurantoin


- renal impairment (leads to loss of efficacy)


- hepatic impairment


- anemia


- electrolyte abnormalities


- asthma


- pregnancy and lactation


- children under 1 month


Interactions:


- probenecid (increased risk of nitrofurantoin toxicity)


- antacids containing magnesium (decreased effectiveness)


- quinolones (antagonistic to each other if both used for UTIs

Patient Ed for Nitrofurantoin


- taking med for required number of days


- report side effects


- take med with milk/food to reduce nausea and vomiting


- avoid antacids


- discoloration of urine (can stain underwear)

Antivirals


Acyclovir: used predominantly treat herpes simplex, herpes zoster (shingles), varicella zoster (chickenpox) infections


- does not cure or prevent further occurrence of blister-like lesion


- topical app effective with initial infection relieve discomfort and shortening healing time


- oral forms most effective in initial treatment of herpes to relieve pain and speed healing of lesions.


*in immunocompromised patients and children, parenteral treatment recommended


- Herpes Zoster (shingles) best treated within 24-72 hours onset of rash (blister-like) or intense pain on skin of one side of trunk or head.


- delayed treatment = PHN postherpetic neuralgia (weeks or months in older adults) = treat with tricyclic antidepressants (e.g. imipramine) or anticonvulsants (e.g. gabapentin)


- Valacyclovir (Valtrex) prodrug converted to acyclovir broken down in body


- same adverse reaction but improved bioavailability means less frequent dosing for valacyclovir. (Famciclovir (Famvir) similar activity but last longer duration of action (dosed less frequently)

Side effects of acyclovir


- impaired renal function (esp with rapid IV infusion)
- lethargy, tremors, confusion, and headache - older adults)


- rash, urticaria, pruritus and photosensitivity


- nausea, vomiting and abdominal pain and diarrhea

precautions or contraindications with acyclovir


- children


- breasfeeding


- renal disease (adjust dose)
- Dehydration


- neurological abnormalities with high doses




Patient Ed: finish full course as prescribed even if feeling better, avoid sexual intercourse when visible genital herpes lesion present and using protection at other times

Neuraminidase Inhibitors


- Oseltamivir (Tamiflu) and zanamivir (Relenza)


- indicated for treatment of uncomplicated acute illness due to influenza types A and B


- both indicated for prophylaxis should not be considered substitute for annual vaccination (gold standard for reducing impact of influenza)


- antivirals adjuncts to prevention and control of influenza


*safety and efficacy for prophylaxis of influenza infection in infants less than 1 year old (Tamiflu) and children less than 7 years for Relenza) not yet established.


- Oseltamivir (oral), Zanamivir (inhalation) - both shorten duration of illness about one day if taken within 48 hours of onset symptoms


- Zanamivir (inhalation) = main side effect is airway irritation and bronchospasm (esp in patietns with COPD)


- Oseltamivir (oral), = causes nausea, vomiting, diarrhea in 1/4, can be lessened by taking meds with food



Ribavirin


- drug with broadest spectrum of antiviral activity = nasal and oral inhalation for treatment of infants and young children with respiratory syncytial virus (RSV) infections


- Adults: used orally or parenterally (IV) treat severe viral infections (ex: lassa fever, Hantavirus, and hepatitis C (in combo with interferon alfa)


Side Effects of ribavirin


- respiratory complications


- hypotension and cardiac arrest


- anemia


- rash and conjunctivitis


Contraindicated: during pregnancy or lactation (serious risk close contact with patients receiving ribavirin inhalation therapy)




Interactions of ribavirin with NRTIs (agents for HIV)


- antagonize antiviral action against HIV


- cause lactic acidosis


- cause hepatic failure

Generic Name = Trade name


Antivirals for herpes infection


acyclovir = Zovirax


famciclovir = Famvir


valacyclovir = Valtrex


zoster vaccine - Zostavax


for influenza


oseltamivir = Tamiflu


zanamivir = Relenza Diskhaler


for RSV


ribavirin = Virazole and Various

AIDS caused by HIV


agents used to treat HIV (antiretrovirals are )


1. protease inhibitors (PIs)


2. nucleoside reverse transcriptase inhibitors (NRTIs)


3. non-nucleoside reverse transcriptase inhibitors (NNRTIs)


4. fusion inhibitors (FIs)


5. integrase inhibitors


6. CCR5 antagonists

Treatment of HIV infection


- HAART highly active antiretroviral therapy used combo with three or more antiretroviral (ARV) agents


Primary approach: disruption of virus at different stages in its reproduction.

Antiretroviral Protease Inhibitors


PIs block activity of HIV enzyme


first PI saquinavir (Invirase) and 8 more


Side effects:


- All PIs associated with GI intolerance (nausea, vomiting and diarrhea)


- Taste alteration in patients receiving ritonavir (liquid form)


- Fat redistribution, hyperlipidemia and insulin resistance


- hyperglycemia, new-onset diabetes mellitus, diabetic ketoacidosis and exacerbation fo existing diabetes


- increased spontaneous bleeding


- indinavir may cause kidney stones (should drink at least 1.5 L per day of water for hydration and prevention)

Nucleoside Reverse Transcriptase Inhibitors


- NRTIs inhibit enzyme responsible for viral replication early in viral life cycle


- Zidovudine (ZDV, Retrovir) first agent approved for treatment of HIV, and 6 more other NRTIs


- NRTIs must be used with combo with other ARVs. (reduce # of pills daily)


*combivir plus Kaletra for pregnancy.


most NRTIs adjusted in patients with renal dysfunction

Side Effects of NRTIs can include


- lactic acidosis and liver dysfunction


- flare up chronic active hepatitis B with abrupt withdrawal of emtricitabine and lamivudine


- bone marrow suppression consisting of anemia and or neutropenia with zidovudine


- pancreatitis with didanosine


- peripheral neuropathy and pancreatitis with didanosine and stavudine


*Abacavir assocaited with hypersensivitiy = can be fatal, prior starting, obtain HLAB5701

Interactions of NRTis include


- alcohol, antacids and iron prep, other drugs that are nephrotoxic





Non-nucleoside Reverse Transcriptase Inhibitors


- inhibit enzyme responsible for viral replication early in viral life cycle


- must be administered in combo with ARVs due to resistance


adverse reactions with NNRTIs


- hepatotoxicity and cutaneous reactions


- psychiatric adverse effects with efavirenz and rilpivirine


Side effects


- CNS symptoms (dizzy, insomnia, abnormal dreams and confusion


INteractions: check with pharmacist (too many)


Dietary considerations


- always check instructions, some given ac and some pc

Fusion Inhibitors


- ARV agent (FIs) block entry of HIV into cells (keep virus from reproducing)
First: Enfuvirtide (Fuzeon)


- administered subcutaneous injection 2x daily


- almost all patients develop local site reactions to enfuvrtide (mild or moderate pain, erythema, itching, induration , nodules, and cysts. (rotate injection site*)

CCR5 antagonists


- block coreceptor required for HIV entry


- Maraviroc (Selzentry) first oral CCR5 antagonist use din conjuction with ARVs


- hepatotoxicity and systemic allergic reaction


*Do not use with St. JOh's wort combo lead to treatment failure and avoid certain ARV combos

Integrase Inhibitors


- Raltegravir (Isentress) first ARV slow advance ment of HIV infection by blocking enzyme needed for viral replication


- most common adverse effects: nausea, headache, diarrhea, and pyrexia


- Rifampin decrease plasma concentrations of raltegravir

Once patients with HIV experience immunosuppression based on decreases in CD4 counts, at risk for opportunistic infections

Chapter 18 Eye medications

Anti-Infectives


Drops: preferred in adults (ointments will cause blurring of vision for 20 mins after)


- ointments preferable to drops in children and patients with poor adherence

Anti-Infectives


In general, topical therapy used for 5-7 days


- prolonged use= overgrowth of non-susceptible organisms (fungi)


- if no improvement in 2-3 days, suspect microbial resistance, inappropriate choice of drug or incorrect diagnosis.

Patient ed for Anti-infectives


- use only as directed, check dosage and frequnecy


- careful instillation into lower conjunctival sac, avoid contamination of tip


- possible hypersensitivity reaction in those with allergies


- discontinuance of med and report any signs of sensitivity


- careful hand washing prevent spread


- not using eyemakeup or contac tlense

Side effects of anti-infectives


- hypersensitivity (conjunctivitis(pinkeye), irritation, local burning, stinging, blurred vision, rash, urticaria


Precautions or contraindications: anyone allergic to drug, viral and fungal diseases of ocular structure


Interactions


- may occur with prolonged use of corticosteroids, can result in secondary ocular infection by suppression of immune response

Interactions of anti-infectives


Antiviral ophthalmic prep used topically in treating


- herpes simplex, keratitis, conjunctivitis include trifluridine (Viroptic) ophthalmic solution


- dose: 1 drop to lower conjunctival sac of infected eye up to 9 times daily at 2-h intervals while awake (21 days per episode)

Anti-Inflammatory Agent


- relieve inflammation of eye or conjunctiva in allergic reactions, burns, irritation from foreign substances


- Corticosteroids


- Nonsteroidal Anti-inflammatory drugs


- Ophthalmic Immunologic agent


- antihistamine or decongestants


- ophthalmic lubricants

Corticosteroids - anti-inflammatory agent


-useful in acute stages of eye injury to prevent scarring, for severe symptoms, when condition is unresponsive to other meds


- should be prescribed cautiously may cause sight-threatening complications when used inappropriately**


- systemic absorption can be minimized by applying gentle pressure on inner canthus of eye follow instillation of corticosteroid ophthalmic drops or ointment

Side effects of corticosteroids


- increased IOP depend on drug, dose, frequency and length of treatment (less likely with flurormetholone)


- reduced resistance to bacteria, viruses, fungi


- delayed healing of corneal wounds, thinning cornea and corneal ulceration


- increased risk for developing cataracts

Precaution/contra corticosteroids


- acute bacterial, viral, or fungal infections


- primary open-angle glaucoma


- pregnancy


- prolonged use

NonSteroidalAnti-Inflammatory Drug (NSAIDS)


- flurbiprofen (Ocufen) and ketorolac (Acular) ophthalmic drops used to treat postoperative inflammation following cataract surgery


- generally not first-line agents for other eye conditions with inflammation but alternative to corticosteroids if contraindication exist


- caution: allergic to aspirin and other NSAIDS,


topical NSAIDS relatively safe with few local or systemic side effects,


Ketorolac may burn during application but alleviated by refrigerating solution betfore use

Ophthalmic Immunologic Agent


- Topical cyclosporine (Restasis) increases tear production in patients whose tear production is presumed suppressed due to ocular inflammation.


- immunosuppressive agent for organ transplant rejection prophylaxis when administered systemically.


- topical cyclosporine demonstrate long-term efficacy and safety in treatment of dry eye disease (other treatment not recommended for long term use)

Side effects of Topical Cyclosporine (ophthalmic immunologic agent)


- mild and transient include ocular burning, itching, stinging, pain and blurred vision




Precautions/Contraindications


- patients with active ocular infections, topical cyclosporine not studied with herpes keratitis

Antihistamine or Decongestants


- blocks histamine receptors in conjunctiva, relieve ocular pruritis (allergic conjunctivitis(


- cause vasoconstriction, relief from minor eye irritation and redness


- many contain preservatives benzalkonium chloride can accumulate in contact lenses causing irritation. (use no more than 72 hours)

Ophthlamic lubricants


- artificial tear solution provide barrier function at level of conjunctival mucosa


- help dilute and flush various allergens and inflammatory mediators


- contain preservatives may cause allergic reaction, stop immediately.


- considered safe and use as often



Patient Ed for Anti-inflammatory drugs


- not rubbing eyes


- follow directions


- lowered resistance to infection. do not use long term


- administration (apply pressure at tear duct inner corner to reduce systemic absorption)


- not wearing contacts if eyes red


- remove lenses prior using products (contacts may be reinserted if eyes not red)


- not suing leftover drug for new eye inflammation- discard drug when no longer needed

Antiglaucoma Agents


- glaucoma: sight-threatening diseases of eye, increased IOP due to obstruction of outflow of aqueous humor.


- cause deterioration of and damage to optic nerve result in vision loss.


Type 1: Acute (angle-closure) glaucoma


- sudden onset of pain, blurred vision and dilated pupil, = medical emergency, uncommon, if left untreated, blindness can result in few hours or days. Treatment: miotics (e.g. pilocarpine), osmotic agents (mannitol) carbonic anhydrase inhibitors (e.g. acetazolamide) and surgery to open pathway for release of aqueous humor.


Type 2: Chronic (open-angle) glaucoma


- much more common, often bilateral, develops slowly over period of years with few symptoms except gradual loss of peripheral visionand possibly blurred vision.


- halos around lights, centralblindness are late manifestations. Treatment: miotics, carbonic anhydrase inhibitors and local beta-adrenergic blocker (timolol Timoptic) eyedrops

First step in glaucoma therapy


- early diagnosis via screening and ensure patient abstains from medications that may exacerbate glaucoma (potent corticosteroids, anticholinergics, and antihistamine)

Antiglaucoma drugs - lower IOP = 5 main categories


1 Carbonic Anhydrase inhibitors Ex dorzolamide (Trusopt) act by decreasing formation of aqueous humor and have diuretic effect


2. Miotics Ex: pilocarpine - act by increasing aqueous humor outflow


3. *Beta-adrenergic blockers: ex: timolol - act by decreasing rate of aqueous humor production


4. Alpha-agonists Ex: brimonidine (Alphagan-P) decrease production of aqueous humor and increase outflow


5. *Prostaglandin analogs: ex: latanoprost (Xalatan) act by increasing aqueous outflow

Carbonic Anhydrase inhibitors CAIs


- acetazolamide: reduce formation of hydrogen and bicarbonate ions (diuretic effect and reduce production of aqueous humor)


- oral acetazolamide (Diamox Sequels) replaced by topical preparations (fewer side effects, used i n adjunctive treatment of open-angle glaucoma or short-term preoperative (IV or regular release abs) to reduce IOP in angle-closure glaucoma given with miotics

Side effects of oral and IV CAIs


- nausea, vomiting, diarrhea and constipation


- thirst, taste alteration; frequent urination


- drowsiness, fatigue, confusion and seizures


- numbness, muscular weakness, tingling with high doses


- blood dyscrasias;electrolyte imbalance


- hepatic and renal disorders (lead to kidney stone)


- photosensitivity

Precautions or contraindications (CAIs)


- COPD


- diabetes


- electrolyte, hematological, hepatic, pulmonary and renal disorders


- sulfonamide hypersensitivity


- pregnancy and lactation


Interactions


- decreased effects of lithium and oral antidiabetics


- increased effects of quinidine, amphetamines and other diuretics


- hypokalemia with thiazides and corticosteroids

Dorzolamide (Trusopt) CAIs


- applied topically to treat open-angle glaucoma


- used adjunct to beta-blockers best combo product with timolol (Cosopt)


Side effects


- burning or stinging and blurred vision


- bitter taste


Caution: those with sulfonamide hypersensitivity


- concurrent ophthalmic and oral CAIs

Miotics Direct-Acting (e.g. pilocarpine)


- cause pupil to contract


- reduce IOP by increasing aqueous humor outflow


- contracting ciliary muscle - blurred vision


- used to treat open-angle glaucoma (third line therapy due to side effects) or short-term treatment before surgery


- Pilocarpine also used after ophthalmic exams in glaucoma patients to "constrict pupil" and counteract the mydriatic (pupil-dilating_ effects of other agents


*Pilopine HS hydrochloride gel advantages: increased duration of effect, less frequent administration, long-tern use with non-compliant patients.


= has cholinergic action and side effects



Side Effects of (pilocarpine) Miotics
- blurred vision and myopia


- twitching, stinging and burning


- ocular pain and headache


- photophobia and poor vision in dimlight


- aggravation of inflammatory processes of anterior chamber of eye


- cataracts and retinal detachment (ciliary muscle spasm)


Systemic Effects (frequent or prolonged use esp in children


- nausea, vomiting, diarrhea


- increased lacrimation, salivation and sweating


- hypotension and bradycardia


- bronchospasm

Precautions or contraindicaitons with pilocarpine


- angle-closure glaucoma with acute inflammation


- history or retinal detachment or retinal degeneration


- acute inflammatory processes


- soft contact lenses in place


- corneal abrasion


Interactions


- topical atropine - reduce effectiveness


Patient Ed


- administer by closing tear duct after instillation


- report side effects for dosage adjustment


- admin at bedtime to reduce side effects


- not driving at night

Beta-Adrenergic Blockers


- Timolol (Timoptic) nonselective beta-adrenergic blocker


- topically lower IOP in open-angle glaucoma (decrease rate of aqueous humor production)


Side effects of beta-blockers: ocular irritation, tearing, conjunctivitis, or diplopia


- transient blurred vision with gel formulation


- aggravation of preexisting cardiovascular or pulmonary disorders (may cause bradycardia, hypotension, dizziness and bronchospasm)


Precautions or contraindications


- bradycardia, heart failure and heart attack


- pateitns receiving oral beta-blockers durg


- asthma and COPD - betaxolol ( Betoptic-S) can be used with caution with bronchospastic pulmonary disease (does not affect pulmonary receptors)


- pregnancy and lactation


- children,


- diabetes and hyperthryoidism


- closed-angle glaucoma

Patient ed beta-adrenergic blockers


- when administer more than one ophthalmic med, allow time interval (at least 5 mins) between meds,


= solution should always be used before gels and suspensions to optimize absorption

Alpha agonists


- Brimonidine (Alphagan-P) is selective alpha2-agonist = decrease formation and increases outflow of aqueous humor


- without causing mydriasis and minimal effects on cardiovascular or pulmonary hemodynamics


- alternative for those whom topical beta-blocker therapy is contraindicated


Side effects


- conjunctival redness, itchy, stinging


dizziness, drowsiness, drymouth, headache


alpha-agonist have potential to enhance CNS depressant effects of ethanol, opiate agonist, anxiolytics, sedatives and hypnotics