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36 Cards in this Set

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Acyclovir (Zovirax) •Action,•Use ADME –SE
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
Acyclovir (Zovirax) caution
•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
Alprazolam (Xanax)
Common Benzodiazepines
Ampicillin
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
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
Antipsychotics
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
Benzodiapzepines
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:
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
Biguanides
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
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
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
Antacids Side Effects Implications
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
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
reason why give Cephalosporin
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
Cephalosporins
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!
Clonazepam (Klonipin)
Common Benzodiazepines
•Long-acting , generally used as an adjunct to other anticonvulsants for absence seizures
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
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
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
Fluoxetine (Prozac)
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
Fluoxetine (Prozac)
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
Fluoroquinolones
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
Gentamycin
•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)
Four main drug groups used for ulcers and reflux
–Acid-neutralizing drugs (antacids)
–H2receptor blockers
–Cytoprotective agents
–Proton pump inhibitors
H2 Blockers
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
Incretin mimetics (Byetta)
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
Incretin mimetics (Byetta)
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!!!!
Insulin formulations all kinds
>?
Lactulose
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
lithium
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
lithium
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
Maalox
Maalox is a brand name antacid containing aluminium hydroxide and magnesium hydroxide to neutralize or reduce stomach acid.
because SE of
Aluminum—constipation,
• Magnesium—diarrhea
they can nutrolize each other
Macrolides
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
Yeast and antibiotics
PCN(Penicillin) Family Interactions
•Real risk of yeast infections in women
Fluconazole (Diflucan)
– Given for persistent yeast infections
Beta lactam rings and resistance
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
Beta lactam rings and resistance
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