Unit 4 Flashcards
Nonabsorbable compound that retains water in intestinal lumen, causing fecal mass to swell and soften
Osmotic laxatives- polyethylene glycol
Most effective for men with mild prostatic enlargement
Tamsulosin
AEs:
*Very well tolerated
Hypoglycemia
Meglitinides
Indications:
Tonic-clonic, simple partial, complex partial seizures
• Drug of choice for partial seizures
• Best for treating tonic-clonic seizures in young children
Bipolar disorder
Trigeminal and glossopharyngeal neuralgias (stabbing pain that occurs along a nerve)
Carbamazepine (Tegretol)
AEs:- Nausea/vomiting -Dyskinesias -Cardiovascular effects -Psychosis -CNS effects
Levodopa
Contraindications:
Don’t use in patients with preexisting liver dysfunction
Stop if pancreatitis is diagnosed during treatment
Pregnancy category D but HIGHLY teratogenic when taken in 1st trimester (neural tube defects, congenital malformations, cognitive dysfunction)
Valproic Acid (Depakene)
Stimulate intestinal motility and increase amount of water and electrolytes within the intestinal lumen by increasing secretion of water and ions into the intestine
Stimulant laxatives
Starting dose for levothyroxine:
1.6mcg/kg/day
AEs:
• Rarely causes side effects
• Acute overdose- thyrotoxicosis can result
o Tachycardia, angina, tremor, nervousness, insomnia, hyperthermia, heat intolerance, sweating
o Can accelerate bone loss and increase risk of AF
Levothyroxine
Advanced nursing implications:
PO sucrose cannot help during hypoglycemia episodes because the medications will impede the absorption in the intestines, must use PO glucose itself.
Check LFT every 3 months r/t potential Liver dysfunction
Alpha-glucosidase inhibitors
Poorly absorbed and cannot be digested by intestinal enzymes and is converted into lactic acid, formic acid, and acetic acid, which exerts a mild osmotic action
Osmotic laxatives- lactulose
Most effective in men who have highly enlarged prostates
Finasteride
MOA:
• Suppression of high-frequency neuronal firing through blockade of sodium channels
• Suppresses calcium influx through T-type calcium channels
• May augment inhibitory influence of GABA
Valproic Acid (Depakene)
MOA:
Prevents breakdown of acetylcholine by acetylcholinesterase- increasing availability of acetylcholine at cholinergic synapses
Donepezil (aricept)
AEs:
GI effects- N/V/indigestion- transient usually (avoid by administering with food and with enteric coated tablet)
Hepatotoxicity- rare but can cause fatal liver failure- usually within first months of therapy
• Don’t use in conjunction with other drugs in children under 2
• Monitor LFTs, use lowest effective dose
Pancreatitis- can be fatal
Hyperammonemia- can occur with or without encephalopathy
Others- rash, weight gain, hair loss, tremor, blood dyscrasias
Valproic Acid (Depakene)
MOA:
• Enhances the action of incretin hormones, which helps blood sugars not elevate as high
• Incretin hormones 1. stimulate glucose-dependent release of insulin. 2. Suppress post-prandial release of glucagon.
• It inhibits DPP-4 enzymes that inactive the incretin hormone action
DPP-4 inhibitors- sitagliptin, “gliptins”
AEs:
Constipation or diarrhea, depending on the agent:
• Aluminum and calcium compounds- constipation
• Magnesium compounds- diarrhea
Sodium compounds raise BP, affect patients with HF
• Also causes eructation and flatulence (liberates CO2)
Aluminum compounds- can bind to tetracyclines, warfarin and digoxin, reducing effects
• Also high in sodium
Antacids
MOA:
binds to base of ulcers and erosions, forming a protective barrier over these areas
o Protects these areas from pepsin, which breaks down proteins, making ulcers worse
Sucralfate
AEs:
Female genitalia fungal infections (Candida infections, yeast infections) *lots of glucose in urine, bacteria breeding ground.
UTI
Increase urination
Hypoglycemia if used in combination of other diabetic medications
In Elderly: can cause postural hypotension and dizziness especially if used with diuretics. Both increase urination and cause dehydration
SLGT-2 inhibitors
MOA:
• Stimulate the pancreas to make insulin (Actively lower blood glucose levels) by binding and inactivating ATP-sensitive potassium channels in the cell membrane = membrane depolarization = calcium influx = insulin excretion
• Long-term use: can target cell sensitivity to insulin
Sulfonylureas- glyburide
AEs:
• Cholinergic effects- N/V/D, dizziness, HA, bronchoconstriction
• CV effects uncommon but can cause bradycardia, fainting, falls (and fractures from falls), requirement of pacemaker placement
Donepezil (Aricept)
AEs:
CNS effects- sedation
Gingival hyperplasia (excessive growth of gum)
Dermatologic effects- morbilliform (measles-like rash) can progress to Stevens-Johnson syndrome or toxic epidermal necrolysis (TEN) (worse with gene variation- HLA-B*1502)
Effects in pregnancy- category D- can lead to cleft palate, heart malformations, fetal hydantoin syndrome (growth deficiency, motor/mental deficiency, microcephaly, craniofacial distortion, etc)
CV effects- if administered IV for status epilepticus- dysrhythmias and hypotension may result
Purple glove syndrome- IV- painful swelling/discoloration in hands and arms
Others- hirsutism, interference with vitamin D- can cause rickets and osteomalacia, interference with vitamin K-dependent clotting factors- can cause bleeding in newborns, liver damage from drug allergy
Phenytoin (Dilantin)
Contraindications:
Don’t use in patients with preexisting hematologic abnormalities
Pregnancy category D
Use caution in patients with HF- monitor sodium levels (hypoosmolarity
Carbamezepine (Tegretol)
MOA:
Selective inhibition of sodium channels
• Causes slow recovery of sodium channels from inactive state back to the active state
• Suppresses action potential- decreasing neuronal firing
• Limited to neurons that are hyperactive, leaving healthy neurons unaffected
Phenytoin (Dilantin)
Contraindications:
Renal impairment or renal insufficiency: excreted unchanged in the kidneys so bad kidneys means toxic levels
Not for individuals with HF
ETOH r/t inhibiting breakdown of lactic acid = increase risk of Lactic acidosis
No cimetidine (h2 blocker for GERD or acid reflux) r/t increase risk of Lactic acidosis
Iodinated Radiocontrast Media: can lead to renal impairment, then increase risk of lactic acidosis
Metformin
Alter stool consistency by lowering surface tension, which facilitates penetration of water into the feces
o Also act on intestinal wall to inhibit fluid absorption and stimulate secretion of water and electrolytes into the intestinal lumen
Surfactant laxatives (Colace)
Starting dose for levothyroxine in elderly patients
25mcg/day
MOA:
• do not prevent overproduction of acid, but does neutralize the acid once in the stomach
o Helps relieve pain by raising gastric pH
• If pH rises >5, can reduce pepsin activity as well
• May also stimulate production of prostaglandins to enhance mucosal protection
Antacids
Once plasma levels reach therapeutic range, small changes in doses produce large changes in plasma levels- small increases in doses can cause toxicity
Sensitive to hepatic metabolism- if too much dose is given, liver’s capacity to metabolize becomes overwhelmed and plasma levels can quickly rise
• Makes it difficult to establish and maintain a dosage that’s safe and effective
Use caution with other CNS depressants- barbiturates, alcohol, other CNS depressants
Phenytoin (Dilantin)
AEs: Upper respiratory infections Headache Sinusitis Inflammation of nasal passage and throat
Pancreatitis (rare)
Potential relationship with hypersensitivity reactions (anaphylaxis, angioedema, and steven’s Johnson syndrome (rare)
DPP-4 inhibitors
Contraindications:
Diuretics can cause dehydration if mixed (*elderly)
Rifampin, phenytoin, phenobarbital will decrease Canagliflozin levels
SLGT-2 inhibitors
Suppresses release of follicle-stimulating hormone from the pituitary gland and suppresses mid cycle luteinizing hormone surge, inhibiting ovulation while also thickening cervical mucus and making the endometrium less hospitable for implantation
Combination OC (estrogen and progesterone)
Short-acting = need to be taken with meals
To avoid hypoglycemia patient needs to eat within 0-30 minutes of taking medication
Meglitinides
MOA:
• Stimulate the pancreas to make insulin (Actively lower blood glucose levels) by binding and inactivating ATP-sensitive potassium channels in the cell membrane = membrane depolarization = calcium influx = insulin excretion (like sulfonylureas)
SHORT-ACTING (sulfonylureas are long-acting)
Meglitinides- repaglinide and nateglinide
AEs:
Upper respiratory infections
Headache
Sinusitis
Myalgia (pain in muscle)
*Heart failure secondary to renal retention of fluid (insulin also promotes fluid retention so when this medication is combined with insulin it is a no-go for HF patients)
Lower risk of hypoglycemia with monotherapy
Can cause ovulation = increase risk for pregnancy
Bladder CA (long-term use of Pioglitazone)
Increases risk of fx in women (long-term use and high doses of Pioglitazone)
Mixed effects on plasma lipids: can elevate cholesterol (bad) & increase HDL (good) and lower triglycerides (good)
Thiazolidinediones
MOA:
Suppresses high-frequency neuronal discharge in and around seizure foci- same as phenytoin
Delayed recovery of sodium channels in their inactivated state
Less SEs than phenytoin
Carbamazepine (Tegretol)
Contraindications: Caution with mild HF Caution with insulin combination r/t HF NO for severe HF NO for individuals with bladder CA or hx of bladder CA
Thiazolidinediones
AEs:
• constipation, nausea, dry mouth
o Can impair absorption of other drugs, especially tetracycline
o Binds with phosphate, may be used in CRF to reduce phosphate levels
Sucralfate
Indications:
***best for partial seizures and tonic-clonic seizures- good for all major forms of epilepsy except absence seizures
Can treat status epilepticus when given IV
Can treat cardiac dysrhythmias
Phentyoin (Dilantin)
MOA:
Acts in reproductive tissue to inhibit 5-alpha-reductase, an enzyme that converts testosterone to dihydrotesterone (DHT), the active form of testosterone in the prostate
• By decreasing DHT availability, promotes regression of prostate epithelial tissue and decreases mechanical obstruction of the urethra
Finasteride
AEs:
Constipation, blurred vision, photophobia, dry eyes, dry mouth, tachycardia, urinary hesitancy, urinary retention, CNS effects- confusion, hallucinations, insomnia, nervousness
Oxybutynin
Acts by altering cervical secretions to act as a barrier to penetrating sperm and modifies endometrium, making it less favorable for implantation
Mini pill (progesterone only)
AEs:
Can intensity dyskinesias caused by levodopa and result in these adverse effects occurring sooner due to elevated levels of levodopa reaching the brain
Carbidopa
MOA:
• Glucose gets transported from the urine back into the blood stream by sodium-glucose co-transporters, the transporter that accounts for most all the reuptake/reabsorption of glucose.
• block the transporters so that glucose cannot be reabsorbed and it makes glucose be peed out (glucosuria)
SLGT-2 inhibitors- canagliflozin, dapagliflozin
AEs:
Minor- HA, n/v/d
Pneumonia due to alteration of upper GI flora and impairment of WBC function
Fractures- decrease in absorption of calcium
Hypomagnesemia- decrease in magnesium absorption
Rebound acid hypersecretion once treatment is stopped
Gastric CA with long-term use- this is not confirmed…
PPIs
AEs: Cramps Gas Abdominal distention Borborygmus (rumbling bowel sounds) Diarrhea *S/E are related to the bacterial fermentation process of unabsorbed carbs
Decrease iron absorption = anemia Liver dysfunction (long-term, high dose therapy)
Alpha-glucosidase inhibitors
AEs:
GI disturbances; loss of appetite, N/V/D
Decrease vitamin B12 and folic acid
Lactic acidosis (rare) (s/s hyperventilation, malaise, myalgia, somnolence) r/t metformin inhibiting breakdown of lactic acid
Metformin
Used for prevention of NSAID-induced gastric ulcers
Misoprostol
MOA:
Prevents decarboxylation of levodopa in small intestine and peripheral tissues, allowing more levodopa to cross the blood brain barrier to be converted to dopamine
Carbidopa
Contraindications:
If sulfonylureas didn’t work for patient neither will these medications r/t same MOA
Liver dysfunction or impairment (metabolized and excreted via the liver/bile) = toxicity = hypoglycemia
NO gemfibrozil (triglyceride lowering medication) r/t it increase metabolism, which can cause hypoglycemia (use a fenofibrate)
Meglitinides
Can affect clopidogrel effects
PPIs
MOA:
• Actives specific receptor type in the cell nucleus called peroxisome proliferator activated receptor gamma (PPAR gamma). Pioglitazone turns on the insulin-responsive genes and it helps regulate carbohydrate and lipid metabolism.
• Decreasing insulin resistance
• Increase glucose reuptake by muscle and fat tissue
• Decreases glucose production by the liver
Thiazolidinediones- pioglitazone and rosiglitazone
Swell in water to form a viscous solution or gel, softening fecal mass and increasing its bulk
o can enlarge growth of colonic bacteria
o Also helps swell fecal mass, stimulating peristalsis by putting pressure on intestinal wall
Bulk-forming laxatives (psyllium, etc)
AEs:-
CNS effects- confusion, lightheadedness, anxiety
-Anticholinergic effects- dry mouth, blurred vision, urinary retention, constipation
Amantadine
MOA:
Relaxes smooth muscle in the bladder neck, prostate capsule, prostatic urethra
• Decreases dynamic obstruction of urethra
• Causes rapid symptom improvement and increased urinary flow
Alpha-adrenergic antagonists (tamsulosin)
Who requires higher doses of levothyroxine?
Pregnant patients
MOA:
Inhibits the binding of acetylcholine to the muscarinic receptors in the detrusor muscle, suppressing involuntary bladder contractions
Results in increased bladder volume voided and a decrease in micturition frequency, sensation of urgency, and number of urge incontinence episodes
Oxybutynin
MOA:
Increases metabolic rate of body tissues:
• Promotes gluconeogenesis
• Increases utilization and mobilization of glycogen stores
• Stimulates protein synthesis
• Promote cell growth and differentiation
• Aids in development of brain and CNS
Levothyroxine
Indications:
All seizure types- first line for partial and generalized seizures
Bipolar disorder
Migraine prophylaxis
Valproic Acid (Depakene)
MOA:
helps protect the stomach by suppressing secretion of gastric acid, promoting secretion of bicarb and cytoprotective mucus and maintaining submucosal blood flow by promoting vasodilation
Misoprostol
Contraindications: Liver problems (metabolized by liver) leads to build-up and toxicity of medication = hypoglycemia Kidney problems (excreted by kidneys) leads to build-up and toxicity of medication = hypoglycemia
No in pregnancy – can cause hypoglycemia in babies
No in lactation – can cause hypoglycemia in babies
No ETOH – (especially first generation) = Disulfiram-like reaction (flushing, palpitations, and nausea)
No Beta-Blockers: suppress insulin release & mask symptoms (tachycardia) r/t hypoglycemia
Caution with non-steroidal anti-inflammatory medications, sulfonamide abx, ETOH , cimetidine = intensify hypoglycemic response
Sulfonylureas
Contraindications:
Use caution with patients with hx of pancreatitis
DPP-4 inhibitors
MOA:
• Acts on the intestines to delay absorption of dietary carbohydrates = reduces the rise in blood sugar after a meal
• The body can only absorb foods if the oligosaccharides and complex carbs are broken down to monosaccharides by alpha-glucosidase (enzyme in the intestine)
• Inhibits the alpha-glucosidase enzyme so that food can’t be broken down and blood sugar can’t elevate
• Decrease peak postprandial glucose levels and A1C
Alpha-glucosidase inhibitors- acarbose and miglitol
MOA:
blocks histamine 2 receptors located on parietal cells of the stomach, reducing secretion of gastric acid
o Suppresses basal acid secretion and secretion stimulated by gastrin and acetylcholine
H2 receptor blockers
AEs:
CNS effects
Neurologic effects- visual disturbances (nystagmus, blurred vision, diplopia), ataxia, vertigo, unsteadiness, HA- common during first few weeks of treatment but tolerance develops with continued use
Hematologic effects- can cause bone marrow suppression (leukopenia, anemia, thrombocytopenia), aplastic anemia, monitor CBC
Hypo-osmolarity- can inhibit renal excretion of water by promoting secretion of ADH
Dermatologic effects- morbilliform rash that can lead to SJS/TEN (worse with gene variation- HLA-B*1502)
Carbamazepine (Tegretol)
MOA:
Inhibits dopamine uptake, stimulates dopamine release, blocks cholinergic and glutamate receptors, increasing dopamine in striatum
Amantadine
AEs:
Dose-related diarrhea, abdominal pain, spotting and dysmenorrhea in women
Misoprostol
Estrogen causes which AEs?
Thromboembolism, HA, nausea
MOA:
• Inhibits glucose production from liver
• Reduces glucose absorption in the gut
• Increase glucose reuptake in the fat and muscle cells by sensitizing insulin receptors
DOES NOT stimulate pancreas to make insulin = does not drive blood glucose down so it does not cause hypoglycemia.
Biguanides- metformin
Can take 6-8 weeks to see reduction in TSH levels at start of therapy
Highly protein bound (almost 100%), so has a prolonged half-life (about 7 days)
• Allows for once daily dosing
• Takes about 1 month to reach steady state- delayed effects at beginning of therapy
Treatment is usually life-long
Levothyroxine
AEs:
Hypotension
Priapism- painful erection lasting 6+ hours
Nonarteritic ischemic optic neuropathy- irreversible blurring or loss of vision
Sudden hearing loss
HA, flushing, dizziness, worsening of OSA
Sildenafil
MOA:
Crosses the blood brain barrier using active transport, where it is converted to dopamine to help lessen effects of PD by increasing dopamine levels
Levodopa
MOA:
• Inhibits H, K ATPase pump, which is the enzyme that generates gastric acid
o Inhibits basal and stimulated acid release
o Not reversible, so effects persist until new enzyme is synthesized, about 3-5 days after stopping the med, can take weeks
PPIs
MOA:
Enhances natural response to sexual stimuli by inhibiting PDE5, increasing cGMP levels in the penis, making erection harder and more long lasting
Sildenafil
Draws water into intestinal lumen, causing fecal mass to soften and swell, stretching intestinal wall and causing stimulation of peristalsis
Osmotic laxatives- laxative salts (magnesium hydroxide, mag citrate, sodium phosphate)
AEs:
Can decrease ejaculate volume and libido
Gynecomastia
Finasteride
AEs:
Nonselective- hypotension, fainting, dizziness, somnolence, nasal congestion
Selective- abnormal ejaculation
Can cause floppy-iris syndrome in men having cataract surgery and can cause blindness
Alpha-adrenergic antagonists (tamsulosin)
AEs:
CNS effects in older patients with renal or hepatic dysfunction
Binds to androgen receptors- can cause gynecomastia, reduced libido, impotence
May cause HA, lethargy, confusion, diarrhea, urticaria, sweating, flushing, other effects
H2 receptor blockers
Nursing Implications:
Accelerated inactivation of OCs and warfarin
Greater induction of metabolism if phenytoin or phenobarbital are used with this drug
grapefruit juice can inhibit metabolism, increasing levels of carbamazepine by 40%)
Carbamazepine (Tegretol)
Use with caution in patients with COPD or asthma- drug can cause bronchoconstriction
Donepezil (Aricept)
Triple therapy for treatment of PUD
PPI, clarithromycin, amoxicillin
Second generations are more potent = lower doses needed
Second generations have WAY LESS drug-drug interaction = have replaced first generations
Sulfonylureas
Drug interactions:
• Reduce absorption- histamine 2 blockers (cimetidine), PPIs, sucralfate, cholestyramine, colestipol, aluminum-containing antacids, calcium supplements, iron supplements, magnesium salts, orlistat
• Accelerate metabolism- phenytoin, carbamazepine, rifampin, sertraline, phenobarbital
• Warfarin- this drug accelerates the degradation of vitamin K-dependent clotting factors- enhances effects of warfarin (dose may need to be reduced)
• Catecholamines- this drug increases cardiac responsiveness to catecholamines (epi, dopa, dobuta), increasing risk of dysrhythmias
• Can increase requirements for insulin and digoxin (may need to increase dosage of these)
Levothyroxine
Advanced Nursing Implications:
narrow therapeutic range- can result in hypothyroidism or toxicity
Be careful if switching brands- bioequivalence may not be the same
• Retest serum TSH 6 weeks after switch
Levothyroxine
AEs:
Can lower already low blood glucose = hypoglycemia
Potential cardiovascular toxicity (ADA does not believe it, and it was linked to first generation tolazamide, state it increases mortality from sudden cardiac death.
Sulfonylureas
Advanced nursing implications:
Women should take calcium and Vitamin D to help avoid fx risk. Bone density should be monitored.
First gen med was taken off market for being severe hepatotoxic LFT (AST & ALT) need to be monitored at baseline and then every 3-6 months. If ALT increases 3 x more than upper limit or if jaundice develops = D/C drug
Thiazolidinediones