pharm exam2

    • -Benign enlargement of prostate resulting in obstruction of urethra.
    • -Overgrowth of epithelial cells (mechanical)
    • -Overgrowth of smooth muscle cells (dynamic)
    • Symptoms: hesitancy, urgency, frequency, dysuria, dribbling, smaller stream, post-void residual, nocturia, straining
  2. BPH tx
    • Treatment options:
    • -Medications (moderate), surgery(severe cases), “watchful waiting”(minimal ss) 
    • Treatment goal:  Relieve symptoms
    • Two main classes: many pt take both
    • **Alpha-1 Adrenergic Antagonists (blockers)- for dynamic
    • **5-alpha Reductase Inhibitors-for mechanical
    • -Recommended drug regimen: combination of drugs
  3. Alpha-1 Adrenergic Antagonists- mech of action, examples
    • -Mechanism of action: relax smooth muscle of the prostatic urethra and bladder neck (trigone and sphincter) by blocking alpha 1 receptors.
    • -Improvement in symptoms is rapid
    • Examples:
    • Terazosin (Hytrin®) and Doxazosin (Cardura®)
    • -Block alpha receptors in blood vessels;vasodilation-decrease BP
    • Alfuzosin (Uroxatral®) and Tamsulosin (Flomax®)
    • -Selective for alpha receptors in prostrate, can raise BP
    • Azosin-A1 blocker
  4. Alpha-1 Adrenergic Antagonists- ADR
    • -Nasal congestion (vasodilation)
    • -Retrograde ejaculation (relaxation of smooth muscle in bladder neck)
    • -Hypotension, dizziness, fainting, nasal congestion for Hytrin® and Cardura®
    • -These drugs often tried before finasteride (Proscar®) because less incidence of sexual side effects; however combination therapy more effective.
    • Drug Interactions- Nitrates, Phosphodiesterase 5 inhibitor (viagra, levitra, cialis), BP meds
  5. 5-Alpha Reductase Inhibitors- mech of action, ADR, examples
    • -Example: finasteride (Proscar®)
    • -Mechanism of action:
    • -Promotes regression of prostatic tissue by inhibiting 5-alpha reductase, the enzyme that converts testosterone to DHT.
    • -Effects seen in 6-12 months.
    • -ADR’s:
    • -sexual dysfunction (5-10%) <libedo, <ejaculation
    • -gynecomastia
    • -decreases prostate specific antigen (PSA) levels
    • -Contraindicated with pregnancy- cat x use precaution-absorbed through skin & inhaled
    • -Note: also marketed under brand name Propecia® for male-pattern baldness
    • -Other example: Dutasteride (Avodart®)-long half life; more complete reduction in DHT
    • if PSA doesnt go down, more likely cancer
  6. Erectile Dysfunction
    • -Erectile dysfunction- impotence
    • -Defined as a persistent inability to achieve or sustain an erection
    • -Associated with chronic illnesses such as DM, HTN, depression
    • -Risk increases with age
    • -Treatment include drugs and implants
    • -Phosphodiesterase 5 (PDE5) Inhibitors
    • -Sildenafil (Viagra)
    • **Used for pulmonary HTN-Revatio
    • -Vardenafil (Levitra)
    • -Talalafil (Cialis)
  7. Erectile dysfunction ADR/interactions
    • -Sildenafil (Viagra)
    • -Relaxes penile and arterial and trabecular smooth muscle (>cyclic GMP)
    • -Drug interactions
    • -Nitrates (GMP)- biggest drug drug interactions
    • -Alpha 1 blockers
    • -Grapefruit juice 
    • -Most common is headache, flushing
    • -hypotension may occur especially in men taking nitrates and alpha blockers
    • -Ischemic optic neuropathy, sudden hearing loss
  8. Bethanechol- use, ADR, caution
    • Urinary retention
    • -Activates muscarinic receptors
    • -Used for urinary retention
    • Adverse effects
    • -Heart-Bradycardia
    • -Gland-Increased sweating, salivation, bronchial secretions, gastric acid secretions
    • Caution:
    • -Asthma, peptic ulcer, GI/GU obstructions
    • Contraction in lung (constriction)
    • GI (increased musccle tone)
    • Bladder (contraction of detrusor)
    • Vascular (relaxation, vasodilation, hypotension)
    • Eye (pupil constrctiona nd ciliary contraction)
    “Overactive Bladder”- cause, tx, drug, mech of action, ADRs
    • Cause: most frequently due to involuntary contraction of the bladder muscle.  Very common in elderly.
    • Treatment: behavioral therapy and medications (often called “antispasmodics”)
    • The drugs:
    • -Oxybutynin (Ditropan®)
    • -Tolterodine (Detrol®)
    • -Solifenacin (VESIcare)
    • -Mechanism of action: block muscarinic receptors of bladder muscle (detrusor) to prevent bladder contraction
    • -ADR’s: anticholinergic side effects
    • Dry mouth, blurred vision, photophobia, hyperthermia, CNS-confusion , dizziness, AMS, psychosis, hot dry flushed skin
  10. furosemide (Lasix®)
    Others: ethacrynic acid (Edecrin®), bumetanide (Bumex®), torsemide (Demadex®)
    • Loop diuretics- most powerful D
    • -Most effective diuretics
    • -Site of action: loop of Henle (kidney)
    • -Mechanism of action: blocks Na and chloride reabsorption>increased osmotic pressure>increased H20 excretion
    • Main uses:
    • -Hypertension
    • -Edema (cardiac, pulmonary, renal, hepatic)used more for edema than HTN
  11. Loop diuretics- ADRs, Allergy, drug interactions
    • ADR’s:
    • -dehydration
    • -hypotension
    • -hypokalemia
    • -ototoxicity (reversible)
    • -hyperglycemia
    • dry mucus membranes, skin turger, confusion (monitor BP)
    • -contraindicated in pregnancy
    • -Allergy: avoid if history of sulfonamide allergy
    • Drug interactions:
    • -digoxin- increases toxicity
    • -aminoglycosides- also ototoxic
    • -antihypertensives
    • -Work well even with renal impairment (even w/ Cr clearance <30)
    • usually on K+ supp, can cause hearing loss
  12. DIURETICS- uses, classifications
    • Promote “diuresis”- movement of fluids and electrolytes out of body.
    • Two major uses:
    • -Hypertension
    • -Edema
    • Classification:
    • -Loop diuretics
    • -Thiazide diuretics
    • -Osmotic diuretics
    • -Potassium-sparing diuretics
  13. hydrochlorothiazide (HydroDIURIL®)- mech of action, uses, allergy
    • Thiazide Diuretics
    • -Generic names end with “-thiazide
    • -Much less diuresis compared to “Loops”
    • -Mechanism of action: same as “Loops” but at the distal convoluted tubule of kidney; dilate blood vessels
    • Major uses:
    • -**Hypertension
    • -Edema due to mild to moderate CHF
    • -Allergy: derived from sulfonamides
    • -Do NOT work well in renal impairment (do not use if cr clear <30)
  14. hydrochlorothiazide- ADRs, Drug interaction
    • ADR’s:
    • -Dehydration
    • -Hypokalemia
    • -Hyperglycemia
    • -Contraindicated in pregnancy
    • Drug interactions:
    • -Digoxin- can increase toxicity
    • -Antihypertensives
    • -NSAIDs+dehyd=kidney failure 
    • -Lithium+dehyd=>lith level
  15. Metolazone (Zaroxolyn)
    • Related drugs (non-thiazide)
    • act like thiazide
  16. spironolactone (Aldactone®)- mech of action, main use
    • Potassium-sparing Diuretics
    • -Amount of diuresis is low
    • Mechanism of action: Blocks action of aldosterone at kidney collecting duct
    • -Aldosterone promotes Na uptake and K secretion
    • Main uses:
    • -With other diuretics for its K-sparing properties
    • -Hypertension (alone, not a first choice)
  17. spironolactone (Aldactone®)- ADRs, drug interactions, other examples
    • ADR’s:
    • -hyperkalemia (EKG, arrythmias, palpations)
    • -many endocrine effects because structurally similar to hormones (gynocomastia)
    • Drug interactions:
    • -potassium supplements
    • -drugs that cause hyperkalemia (ie. ACE inhibitors, ARBs)
    • Other examples:
    • -Triamterene (Dyrenium®) and Amiloride (Midamor®)
    • -Both block sodium-potassium exchange in distal nephron
    • -May cause hyperkalemia
  18. omannitol (Osmitrol®)-mech of action, main use, ADRs
    • Osmotic Diuretics
    • Mechanism of action: creates an osmotic force within lumen of proximal convoluted tubule of kidney which pulls water into lumen of tubule.
    • -Causes no significant effect on excretion of electrolytes (sodium, chloride, potassium)
    • Main uses:
    • -Preserve urine flow in impending renal failure
    • -Reduce intracranial pressure
    • typically only used in ICU
    • ADR’s:
    • -Can cause edema! Discontinue if signs of pulmonary edema or if renal failure develops.
  19. Electrolytes-Potassium
    • -Most abundant intracellular cation
    • -Helps with nerve conduction and acid-base balance, maintain electrical muscle activity
    • -Hypokalemia-cramps, arrhythmias, insulin
    • -Potassium salts usually SR- less N/V/D
    • -Administer IV slowly
    • -Assess renal function and EKG changes
    • -Hyperkalemia-tissue trauma, acidosis , elevated T waves, PR prolonged, cardiac arrest
    • -Hyperkalemia S/S-Confusion, weakness or heaviness of legs, numbness, tingling of hands, feet, lips
  20. Electrolytes- Magnesium
    • Hypomagnesemia
    • -Caused by diarrhea, hemodialysis, chronic alcholism, others
    • Treatment
    • -Po magnesium gluconate or hydroxide (diarrhea)
    • -IV magnesium sulfate (no diarrhea
    • -Caution with replacement in renal insuffiency can cause kidney failure
Card Set
pharm exam2
urinary tract & renal disorders