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36 Cards in this Set
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Acyclovir (Zovirax) •Action,•Use ADME –SE
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Herpes and Varicella
•Prototypes: acyclovir (Zovirax), •Action –Interferes with DNA replication •Use –Needs to be initiated within 24 hr of onset of s/s –T ½ is 2 ½ hr, need to take q4h while awake for acute infections, chronic maintenance dose is bid –Available in PO, IV, and topical forms |
ADME
–Poor absorption PO (20%) but can reach therapeutic blood levels, widely distributed even to CSF and the vesicles of the herpetic lesions –Concurrent admin of probenecid (Benemid) increases serum levels –SE •GI sx, dizziness •Phlebitis or acute renal failure can occur with rapid administration IV |
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Acyclovir (Zovirax) caution
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•Cautions
–Patients with dehydration or renal impairment are at risk for nephrotoxicity •Monitor BUN and creatinine levels during therapy –IV administration over at least 1 hr to prevent renal crystals from forming, rotate infusion sites to prevent phlebitis |
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Alprazolam (Xanax)
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Common Benzodiazepines
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Ampicillin
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Aminopenicllins (broader spectrum)
• Prototype: Ampicillin, • Indications – Also useful in selected gram-negative bacteria so broader spectrum but not penicillinase resistant – Protected from beta-lactamase when potassium clavulanate added (Augmentin) • Only have to take tid instead of qid |
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Inhibition of nucleic acid synthesis
– Antivirals |
•Viral infections more difficult to treat because the virus has reached is peak of replication before symptoms appear
•Many viral conditions are treated in a chemoprophylactic way •Viruses replicate in human cells, the drugs that inhibit replication of their enzymes also affect the host cells and may be toxic |
•Used alone or in combination
•Indications –Herpes simplex, herpes zoster, genital herpes, varicella –Influenza –RSV –HIV |
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Antipsychotics
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Primary use schizophrenia
does not cure relieves distressing hallucinations, bizarre behaviors, thought disruptions, agitation Different drugs impact different symptoms Positive Symptoms (Sees or hears things that are not there (added to psyche)) Negative Symptoms (Flat affect, poor interaction,withdrawal) Cognitive Symptoms |
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Benzodiapzepines
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Widely prescribed for anxiety, insomnia and
seizures • Lower fatality rates than barbiturates • Lower potential for abuse • More favorable SE profile • Fewer drug-drug interactions Potential for abuse • Schedule II and III |
Two benzodiazepine receptors
•BZ 1 located in the cerebellum •Mediate anxiety •BZ 2 locatedin the basal ganglia and hippocampus •Muscle relaxation and cognitionBenzodiazepines: |
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Benzodiapzepines
Anticonvulsant Drugs Seizure Medications Sedative |
•Control symptoms but not curative
•Increases of symptoms may be sign of developing tolerance •Withdrawal if stopped abruptly, need to taper off over 2 weeks •Orals have minimal CV SE; same drug given IV can have profound CV effects |
Respiratory patients: can exacerbate apnea and airway obstruction issues.
•Typically minor respiratory depression Can produce amnesia of events while dose on board •Problems in judgment •Problems be accuracy of memory |
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Biguanides
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Biguanides
•Metformin/Glucophage –Decreasing hepatic production of sugar and enhances peripheral utilization of glucose by skeletal muscle. –No insulin release from the pancreas, nor does it cause hypoglycemia –Monitoring renal function is vital –Can be used with insulin and sulfonylureas –Major problem: lactic acidosis •inhibits the metabolism of lactic acid, inducing a metabolic acidosis. 50 % mortality rate, occurs almost exclusively in people with renal insufficiency |
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Biscodyl (Ducolax) Action •ADME •Caution
Stimulant Laxatives |
Prototypes: bisacodyl (Dulcolax,
•Action –Work on intestinal muscles and secretory cells to stimulate motility and fluid movement •ADME –Onset commonly 6-8 hr, cramping and watery discharge •Caution –Associated with fluid loss, can lead to dependency |
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Calcium Carbonate (TUMS)
Antacids • ADME |
don't worry about over taking calcium because it has to take 6-10 TUMS per day to get
calcium |
Antacids
• ADME – Rapid onset, lasts 20-40 min if fasting but can be extended up to 3 hr if taken 1 hr pc – Small amt absorbed, remainder broken down and excreted in feces • Drug-drug interactions – Reduces absorption of many drugs (chelation) • timing is important • because stomach less acidic, enteric coating dissolves faster releasing drugs earlier than expected |
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Antacids Side Effects Implications
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Side Effects
• Aluminum—constipation, bone demineralization • Calcium—gastric acid hypersecretion, constipation, kidney failure, Ca levels • Magnesium—diarrhea, K and Mg levels • Sodium—sodium overload (CV workload),gastric acid hypersecretion |
Implications
• Long-term use can cause kidney failure • Shake liquid suspensions before use • Check expiration dates—effectiveness decreases with age of product • Have to take 6-10 TUMS per day to get calcium |
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Cephalosporin
Inhibit cell wall synthesis (bactericidal) Allergic reactions |
Allergic reactions
– Rashes to anaphylaxis—penicillins are most common causative agent along with cephalosporins and sulfonamides • 10% with allergy to PCN also react to cephalosporins |
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reason why give Cephalosporin
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Over time bacteria have developed enzymes
to dismantle this central molecular component of the drug.: – Bacteria can produce enzymes (ß-lactamase or penicillinase) that destroy the ß-lactam ring. • Therefore can be resistant to many penicillins and |
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Cephalosporins
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Cephalosporins
•Chemical modifications of the penicillin structure (Also inhibit cell wall synthesis) •Divided into generations –First—primarily active against gram + –Second—increased activity against gram – –Third—more active against gram –than gram + –Fourth—like 3rdgeneration, but more resistant to beta-lactamas |
SE
–GI sx –Superinfections esp C.difficle! –10% allergic rxn (cousin of PCN) –Candidiasis –Rash, pruritus, edema •Many members all with names that look and sound alike! |
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Clonazepam (Klonipin)
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Common Benzodiazepines
•Long-acting , generally used as an adjunct to other anticonvulsants for absence seizures |
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Diazepam (Valium) Indication Action
ADME and SE |
Benzodiazepines
Prototype: diazepam (Valium) Indication •Anxiety, sedation, relief of muscle spasm, management of acute alcohol withdrawal, prep for surgical and/or diagnostic procedures Action •Wide range of selectivity for CNS effects •Bind to specific benzo receptors and potentiate gamma-aminobutyric acid (GABA),an inhibitory neurotransmitter |
ADME
•Well absorbed and widely distributed •High density of BZ receptors in limbic system •Many of the metabolites are CNS depressants, can become excessive with prolonged use SE •Drowsiness, hiccups, loss of dexterity •Less common—GI sx, blurred visionDiazepam |
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Diazepam Adverse reactions
Drug-drug interactions Toxicity Cautions |
Adverse reactions
•Behavioral problems (mostly in children) •Insomnia, hallucinations, apprehension Drug-drug interactions •Other CNS depressants, especially ETOH Very irritating to vein when given IV |
Toxicity
•High margin of safety •Combined overdose is a problem Cautions •Can worsen depression •Significant incidence of suicidal tendencies •May cause resp depression in COPD •Careful with glaucoma, renal failure, older adultsBenzodiazepine |
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Erythromycin ( Emycin)
Inhibit protein synthesis(bacteriostatic) |
Macrolides
• Prototypes: erythromycin, • Inhibit protein synthesis (bacteriostatic) • Properties – Oral and topical preparations – Drug of choice for many respiratory infections – One of the least toxic, few allergies • SE GI sx can affect compliance |
• Indications
– Legionella, bordetella, diptheria, chlamydia • Drug interactions with digoxin, warfarin, theophylline, clindamycin, carbamazepine • Food decreases absorption |
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Fluoxetine (Prozac)
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SSRIs
Prototype: fluoxetine (Prozac) Action Blocks reuptake of serotonin in the CNS ADME Can take 2-4 weeks to reach therapeutic effect Indication depression without anxiety overlay |
12SSRIs
Prototype: fluoxetine (Prozac) Action Blocks reuptake of serotonin in the CNS ADME Can take 2-4 weeks to reach therapeutic effect Indication depression without anxiety overlaySide Effects Onset queasy, feel ―fuzzy‖ more active dreams Longer term dry mouth, constipation Anorexia, weight loss Sexual dysfunction Anxiety, HA, insomnia, nervousness, diarrhea, tremor, pruritus |
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Fluoxetine (Prozac)
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Drug-drug interactions
MAOIs, St. John’s Wort Causes Dilantin, theophylline toxicity Increases concentration of beta blockers Need to monitor LFTs Don’t use if hepatic impairment Don’t mix with alcohol |
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Fluoroquinolones
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Fluoroquinolones
• Prototype: ciprofloxacin (Cipro) • Synthetic, broad spectrum, bactericidal by altering bacterial DNA • Wide distribution in body – Agent of choice for pseudomonas, anthrax • Not effective vs strep pneumonia |
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Gentamycin
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•Prototype: gentamicin (Garamycin)
•Potent bactericidals, interferes with bacterial RNA which leads to cell death •Indications –Serious gram –infections (pseudomonas, e. coli) –Used in conjunction with PCNs, cephs, or vanco –Absorption: good IM, poor PO –Wide distribution except for eye and CNS •Opthalmic solution and ointment available |
•SE
–Nephrotoxicity:kills renal tubules –Ototoxicity:kills sensory cells of inner ear •Overdose –Neuromuscular blockade •Check drug levels (peak and trough) |
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Four main drug groups used for ulcers and reflux
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–Acid-neutralizing drugs (antacids)
–H2receptor blockers –Cytoprotective agents –Proton pump inhibitors |
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H2 Blockers
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Prototype: cimetidine (Tagamet)
–Others: Zantac, Pepcid, Axid •Action –Prevent histamine from stimulating H2 receptors on gastric parietal cells, thus reduces volume of gastric acid secretion –Relieves pain from hyperacidity •Indication –Treatment andprevention of PUD, reflux diseases, hypersecretion of acid |
Availability
–Tablets, easier to take than liquid, less frequent dose •Can be taken with or without food, single hs dose is common –Parenteral for IV use •SE –Anorexia, n/v, diarrhea, constipation, confusion Drug-drug interaction – If taken simultaneously with antacids will have reduced effect – Reduces hepatic metabolism of many other drugs • E.g., beta blockers, oral anticoagulants, theophylline, antifungals, TCAs • Toxicity – Tachycardia, changes in mental status |
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Incretin mimetics (Byetta)
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IncretinMimeticsExenitide/Byetta
•Can be used in conjunction with sulfonylureas, metformin and now insulin ( new 2011) •Injection, but is NOT insulin, –Synthetic analogue to human incretin, GLP-1 –Glucagon-like peptide-1, made by small intestine in response to food in GI tract –Augments insulin secretion so long as glucose is present –The “incretin effect” accounts for 60% of total insulin release following a meal –Endogenous incretins are rapidly degraded by GI enzyme, DDP-IV (dipeptidyl pepsidase-IV) |
38Incretin MimeticsExenitide/Byetta
•GLP-1 has multiple effects on body –Brain: increased satiety, reduced appetite, eat less, lose weight –Alpha cells of pancreas: decreased post-prandial glucagon secretion –Liver: decreased hepatic production of sugar –Beta cells: enhanced glucose-dependant insulin secretion –Stomach: decreased gastric emptying which translates into eating less food, lose weight |
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Incretin mimetics (Byetta)
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39GLP-1 Agonists
•Insulin production: signals the pancreas to make the right amount of insulin—then stops after blood sugar levels get closer to normal •Sugar production: helps stop the liver from producing too much sugar when you don't need it —helping avoid high blood sugar levels •Sugar digestion: helps slow down the rate at which sugar enters the bloodstream —also helping to avoid high blood sugar spikes |
40Incretin MimeticsExenitide/Byetta
•taken SQ before breakfast and dinner. –5mcg or 10 mcg BID –Check a finger-stick blood sugar 2 hours after these meals will help determine if the med is working. –On the + side, patients showed a nice weight loss with exenitide –Significant n/v as primary side effect –If taking with sulfonylurea, hypoglycemia possible Hot off the PRESS! •Once a week exentide! •Injection that must be reconstituted immediately before giving it –Cannot be pre-mixed! –Patient needs injection education •Perhaps even better HgA1C reduction than 2-3 x a day! •WEIGHT LOSS!!!! |
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Insulin formulations all kinds
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>?
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Lactulose
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Prescription Laxative
Prototype: lactulose (Chronulac, Duphalac) •Action –Consists of sugars which are metabolized to acids to produce an osmotic effect with increased fluid accumulation, distention, peristalsis –Also decreases serum ammonia levels in persons with chronic liver disease (e.g., cirrhosis) •ADME –Bowel movement within 24-72 hr –Minimal absorption |
•Indication
–Chronic constipation that does not respond to OTC bulk laxatives •SE –Dose-related flatulence and intestinal cramps, gas, belching –Excessive doses may produce nausea and diarrhea |
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lithium
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Tx for Mania
DOC: lithium Action Not well known, theory that it accelerates the destruction of serotonin, dopamine, and NE Na in cells of manic clients increases by 200%, lithium actively transported in with Na but can’t be pumped out, thus may stabilize cell membranes |
Indication
Manic-depressive illness Effect Decreases number and severity of episodes, effective in 80% of cases ADME Response in 1-3 wk 16Lithium SE Dry mouth, nausea, diarrhea, thirst, drowsiness, weight gain, sleeplessness in early weeks Higher blood levels produce more weight gain, metallic taste, altered taste in food, HA, pruritus, edema of hands and feet Very low margin of safety Therapeutic level: 0.8-1.2 mEq/L Toxic level: 1.5-2.0 mEq/L |
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lithium
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Serum Levels
Increased by diarrhea, diuretics, dehydration, low salt diets, high fevers, strenuous exercise Decreased by High salt intake, high intake of sodium bicarbonate, pregnancy |
pregnancyLithium
Drug-drug interactions Doesn’t take much to alter levels to nontherapeutic or toxic ranges Diuretics—alter Na levels Secretion of thyroid hormone inhibited may need replacement therapy 17Overdose and toxicity Even in normal doses: much GI upset anorexia, bloating, slight nausea Early: drowsiness, diarrhea, nausea worsen Late: vomiting, muscle weakness, ataxia, polyuria, circulatory collapse |
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Maalox
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Maalox is a brand name antacid containing aluminium hydroxide and magnesium hydroxide to neutralize or reduce stomach acid.
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because SE of
Aluminum—constipation, • Magnesium—diarrhea they can nutrolize each other |
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Macrolides
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Macrolides
• Prototypes: erythromycin, azithromycin (Zithromax), clarithromycin (Biaxin) • Inhibit protein synthesis (bacteriostatic) • Properties – Oral and topical preparations – Drug of choice for many respiratory infections – One of the least toxic, few allergies • SE GI sx can affect compliance |
Macrolides
• Indications – Legionella, bordetella, diptheria, chlamydia • Drug interactions with digoxin, warfarin, theophylline, clindamycin, carbamazepine • Food decreases absorption |
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Yeast and antibiotics
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PCN(Penicillin) Family Interactions
•Real risk of yeast infections in women |
Fluconazole (Diflucan)
– Given for persistent yeast infections |
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Beta lactam rings and resistance
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Penicillins
• Prototypes: penicillin G, penicillin V, methicillin • Action – Act on the developing bacterial cell wall making it susceptible to osmotic pressure and it explodes – Most effective against gram-positive bacteria – Contain a molecular structure called a betalactam ring which is essential to its antibiotic abilities (called a ß-lactam group) |
Bacteria can produce enzymes (ß-lactamase or
penicillinase) that destroy the ß-lactam ring. • Therefore can be resistant to many penicillins and some cephalosporins that have this central ring |
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Beta lactam rings and resistance
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Aminopenicllins (broader spectrum)
• Prototype: Ampicillin, amoxicillin • Indications – Also useful in selected gram-negative bacteria so broader spectrum but not penicillinase resistant – Protected from beta-lactamase when potassium clavulanate added (Augmentin) • Only have to take tid instead of qid |
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