Drugs acting on gentiourinary system

1. Drug Presentation on
Drugs acting on
Genitourinary System
Ms Alisha Talwar

2. Genitourinary system
 The genitourinary system or urogenital system is
the organ system of the reproductive organs and the urinar
system. These are grouped together because of their proximity
to each other, their common embryological origin and the use
of common pathways, like the male urethra

3. Drugs acting on Genitourinary
system
1. Antidiuretics
2. Diuretics
3. 5 alpha- reductase inhibitors for prostate enlargement
4. Alpha blockers for prostate enlargement
5. Antiinfectives in genitourinary medicines
6. Antigout agents
7. Ketoanalogues, amino acids
8. Spermicides
9. Urologicals

4. Anti- diuretics or Anti- Aquarectics
 An antidiuretic is a substance that helps to control fluid balance
in a human body by reducing urination, opposing diuresis. Its
effects are opposite that of a diuretic.
 Hormone (protein) secreted by posterior pituitary
(neurohypophysis)
 The antidiuretic hormone class includes vasopressin (ADH),
argipressin, desmopressin, lypressin, ornipressin, oxytocin, and
terlipressin. Miscellaneous others include chlorpropamide and
carbamazepine.
 Mechanism of action: It enhances water reabsorption from
the collecting ducts, it activates the V2 receptors on the cell
membrane thereby in creases the water permeability of the
cells.

7. Indications of Vasopressin
 Diabetes Insipidus
 Night time bed wetting
 Hemophilia
 Dehydration
 Von Willebrand's Disease
 Ventricular fibrillation
 Gastrointestinal Hemorrhage

8. Contraindications
 Bright's disease.
 Asthma
 Kidney disease
 Congestive heart failure
 Hardened arteries
 Migraine headaches
 Seizures
 Coronary artery diseases
 Circulation problems

9. Side effects
 Transient headache and flushing: frequent
 Local Application: Nasal irritation, congestion, rhinitis,
 ulceration, epistaxis
 Systemic Side effects: belching, nausea, vomiting,
 abdominal cramps, pallor, urge to defecate, backache
 in females (uterine contraction)
 Fluid retention, hyponatremia
 Bradycardia, increased cardiac afterload, precipitate angina

10. Nursing Considerations
 Monitor BP and weight throughout therapy. (Dose used to
stimulate diuresis has little effect on BP.) Report sudden
changes in pattern to prescriber.
 Advise patient to drink 1– 2 glasses of water at time of
administration to minimize side effects (blanching of skin,
abdominal cramps, nausea).
 Inform patient that these side effects are not serious and
usually disappear in a few minutes.
 Caution patient to avoid concurrent use of alcohol while taking
vasopressin.
 Patients with diabetes insipidus should carry identification at all
times describing disease process and medication regimen.

11. Research evidence
The role of oxytocin and vasopressin in central nervous system activity and mental disorders
 Oxytocin and vasopressin, "peptides of love and fear", except for their classic role in control
of labor and breastfeeding and blood pressure regulation, are also implicated in various
processes like sexual behaviours, social recognition and stress response. These hormones
seems to be essential for appropriate and beneficial social interactions, play a very
important role in maternal care and closeness, promote general trust and cooperation and
prolong social memory. They also play a very important role in modulating fear and anxiety
response, especially by regulating the hypothalamic-pituitary-adrenal axis and amygdala
activity by its projections to the brain stem and hypothalamic structures. Both hormones,
particularly oxytocin, appears to be activating sexual behaviour or is responsible for
increased sexual arousal. Evidence from clinical trials suggests their potential role in
pathogenesis of schizophrenia, depression, autism and addiction together with possible
therapeutic use in the above conditions. In schizophrenia, patients with higher peripheral
oxytocin levels showed less severe positive, general and social symptoms and better
prosocial behaviours. Literature suggests that exogenous oxytocin may be effective as an
adjunctive therapy for that illness. Some data suggest that naturally occurring
autoantibodies reacting with oxytocin and vasopressin are involved in depression, eating
disorders and conduct disorder genesis.

12. Research Evidence
 Terlipressin and albumin in patients with cirrhosis and type I
hepatorenal syndrome.
 PURPOSE:Hepatorenal syndrome (HRS) is a pre-renal-like dysfunction that
generally onsets in cirrhotic patients presenting ascites. We investigated the
improvement of renal function in subjects with hepatorenal syndrome after
terlipressin administration and the survival times after this treatment. Fifty-
two patients affected by cirrhosis, with diagnosis of hepatorenal syndrome
were treated with intravenous terlipressin plus albumin (group A) or with
albumin alone (group B). Liver and renal function, plasma renin activity, and
aldosterone plasma levels were monitored. RESULTS:Patients from group A
showed a significant improvement (p < 0.001) of renal function valued by
creatinine rate compared with the results obtained in group B. The probability
of survival was higher in the group A (p < 0.0001).CONCLUSIONS:Our
results seem to confirm that the administration of terlipressin plus albumin
improves renal function in patients with cirrhosis and type I HRS and that a
reversal of hepatorenal syndrome is strongly associated with improved
survival.

13. Diuretics

14. Classes of Diuretics
 Thiazide and Thiazide-like Diuretics
 Loop Diuretics
 Carbonic Anhydrase Inhibitors
 Potassium-Sparing Diuretics
 Osmotic Diuretics
Function of diuretic agent
 Increase the amount of urine produced by the kidneys
 Increase sodium excretion

15. Indications for Diuretic
 Edema associated with congestive heart failure
 Acute pulmonary edema
 Liver disease (including cirrhosis)
 Renal disease
 Hypertension
 Conditions that cause hyperkalemia

16. Sites of action of Diuretics

17. Thiazide and Thiazide-Like Diuretics
 Hydrochlorothiazide (HydroDIURIL)
 Chlorothiazide (Diuril)
 Bendroflumethiazide (Naturetin)
 Benzthiazide (Exna)
 Hydroflumethiazide (Diucardin)
 Methyclothiazide (Aquatensen)
 Polythiazide (Renese)
 Trichlormethiazide (Diurese)

18. Contd..
Actions
 Action is to block the chloride pump
 Keeps chloride and the sodium in the tubule to beexcreted in
the urine, thus preventing the reabsorption of both in the
vascular system
Indications
 Treatment of edema associated with CHF, liver, orrenal
disease
 Monotherapy or adjuncts for the treatment ofhypertension

19. Contd…
 Pharmacokinetics
• Well absorbed for the GI tract, metabolized in the
liver and excreted in the urine.
 Contraindications
• Allergy to thiazides or sulphonamides
• Fluid and electrolyte imbalances, and renal and liver disease
• Bipolar disorders
• Pregnancy and lactation

20. Contd…
 Caution
• Gout
• Systemic lupus
• Diabetes
• Hyperparathyroidism
 Adverse Effects
• Hypokalemia
• Decreased calcium excretion
• Altered blood glucose levels
• Urine will be slightly alkalinized

21. Question
What is the action of thiazide diuretics?
A. Blocks the chloride pump
B. Blocks the sodium pump
C. Blocks the potassium pump
D. Blocks the carbonic anhydrase pump

22. Answer
A. Blocks the chloride pump
Rationale: Thiazide and thiazide-like diuretics act to block
the chloride pump. Chloride is actively pumped out of the
tubule by cells lining the ascending limb of the loop of
Henle and the distal tubule.

23. Loop Diuretics
 Furosemide (Lasix)
– Most commonly used
 Bumetanide (Bumex) and Torsemide (Demadex)
– New drugs,more powerful than Lasix
 Ethacrynic acid (Edecrin)
– First loop diuretic introduced, used less frequently in
the clinical setting

24. Contd…
 Action- Block the chloride pump in the ascending loop of
Henle. This causes reabsorption of sodium and chloride
 Indications
• Acute CHF
• Acute pulmonary edema
• Edema associated with CHF
• Edema associated with renal or liver disease
• Hypertension

25. Contd..
 Pharmacokinetics- Metabolized and excreted primarily
through the urine
 Contraindications
• Allergy
• Electrolyte depletion
• Anuria
• Severe renal failure
• Hepatic coma
• Pregnancy and lactation

26. Contd…
 Caution- SLE, gout, and diabetes mellitus
 Adverse Effects
• Hypokalemia
• Alkalosis
• Hypocalcemia

27. Carbonic Anhydrase Inhibitors
 Action
– Block the effects of carbonic anhydrase; slow down the
movement of hydrogen ions
– More sodium and bicarbonate are lost in the urine
 Indications
• Adjuncts to other diuretics
• Glaucoma

28. Contd..
 Pharmacokinetics
• Rapidly absorbed and widely distributed
• Excreted in the urine
 Contraindications
• Allergy
• Angle closure glaucoma
 Adverse Effects
• Metabolic acidosis
• Hypokalemia
• Paresthesias of extremities, confusion, drowsiness

29. Question
Please answer the following statement as true or false.
The loop diuretics cause the body to excrete a copious
amount of potassium-rich urine.

30. Answer
False
Rationale: The loop diuretics have a similar effect in the
descending loop of Henle and in the distal convoluted
tubule, resulting in the production of a copious amount of
sodium-rich urine.

31. Potassium Sparing Diuretics
 Action
• Cause a loss of sodium while retaining potassium
• Block the actions of aldosterone in the distal tubule
 Indications
• Adjuncts with thiazide or loop diuretics
• Patients who are at risk for hypokalemia
 Pharmacokinetics
• Well absorbed, protein bound, and widely distributed
• Metabolized in the liver and excreted in the urine

32. Contd…
 Contraindications
• Allergy
• Hyperkalemia, renal disease, or anuria
• Patients taking amiloride or triamterene
 Adverse Effects – Hyperkalemia

33. Osmotic Diuretics
 Action – Pull water into the renal tubule without sodium loss
 Indications
• Increased cranial pressure or acute renal failure due to
shock, drug overdose, or trauma
 Pharmacokinetics
1. Freely filtered at the renal glomerulus, poorly reabsorbed
by the renal tubule
2. Not secreted by the tubule
3. Resistant to metabolism

34. Contd..
 Contraindications
• Renal disease and anuria
• Pulmonary congestion
• Intracranial bleeding, dehydration
• CHF
 Adverse Effects – Nausea, vomiting, hypotension, light-
headedness, confusion, and headache

35. Question
How do carbonic anhydrase inhibitors work?
A. Slow down the reabsorption of sodium
B. Speeds up creation of sodium bicarbonate
C. Balances acidic and alkaline solutes in urine
D. Slows down the movement of hydrogen ions

36. Answer
D. Slows down the movement of hydrogen ions
Rationale: Diuretics that block the effects of carbonic
anhydrase slow down the movement of hydrogen ions.
As a result, more sodium and bicarbonate are lost in the
urine.

37. Nursing Considerations
 Monitor BP often and assess for orthostatic hypotension;
periodically assess weight as an index of fluid retention.
 Lab tests: Monitor serum electrolytes, uric acid, blood glucose,
BUN, and creatinine periodically throughout the course of
therapy.
 Monitor coagulation parameters and lithium levels in patients on
concurrent anticoagulant and/or lithium therapy.
 Check weight at least weekly and report abrupt gains or losses to
physician.
 Understand the risk of orthostatic hypotension.
 Report symptoms of hypokalemia (see Appendix F) or hearing
loss immediately to physician.
 Monitor blood glucose for loss of glycemic control if diabetic.
 Do not breast feed while taking this drug without consulting
physician

38. Diuretics

39. Ketoanalogues

40. Ketosteril
 Mechanism of Action-It can provide essential amino acids
and reduce the intake of amino nitrogen. It can utilize the
nitrogen in non-essential amino and turn them into amino
acids so as to reduce the production of urea nitrogen. It can
reduce building up of uremic toxins in blood significantly.
 Dosage / Direction for Use-Adults (70 kg/body
weight): 4-8 tablets 3 times daily during meals

41.  Indications- Prevention and therapy of damages due to faulty
or deficient protein metabolism in chronic renal insufficiency in
connection with limited protein food of ≤40 g/day. Amino acid
deficiency, Incontinence, Asthma, Paracetamol poisoning,
Allergies, Radiation side effects, Alcohol, Copper poisoning,
Diaper rashes, Paracetamol over dosage, Depression
 Contraindications
 Hypercalcemia
 Disturbed amino acid metabolism.
 In case of hereditary phenylketonuria, it has to be taken into
account that Ketolog contains phenylalanine.
 Adverse Reactions
 Hypercalcemia may develop.

42. Nursing Considerations
 Protein intake to be reduced
 A protein-restricted diet can prevent/reduce waste load on
the kidneys so kidney function can be maintained. However,if
you do not have enough consumption of protein, you may
develop malnutrition.
 The keto acids in ketosteril are amino acids without nitrogen,
inside the body they bind with body’s nitrogen and forms
proteins,so you are less prone to develop malnutrition.
 Assess the serum creatinine and BUN levels. High creatinine
and BUN levels result from impaired kidney structure and
reduced renal function. Ketosteril only can reduce the
production of wastes in body to lower levels of creatinine and
BUN.

43. Anti-Gout
 Gout is a familial metabolic disease characterized by recurrent
episodes of acute arthritis due to deposits of monosodium urate
in joints and cartilage.
 Formation of uric acid calculi in the kidneys may also occur.
 Treatment of gout is aimed at relieving the acute gouty attack
and preventing recurrent gouty episodes and urate lithiasis.
 Common drugs are- Colchicine, Allopurinol, Febuxostat,
Lesinurad, Pegloticase, Probenecid, Rasburicase.
 Mechanism of Action- Inhibits reabsorption of uric acid at
the proximal convoluted tubule. Also, inhibits renal tubular
secretion of weak organic acids, such as penicillins.

44.  Indications
• Acute gouty arthritis
• For the prophylaxis of recurrent episodes of gouty arthritis
 Contraindications-Blood dyscrasias, concurrent high-dose
aspirin therapy, severe renal impairment, uric acid calculi
 Adverse Effects : Nausea, vomiting, abdominal pain,
Headache, Anorexia, Lower back pain, rashes, flushed face and
gingivitis.

45. Nursing Responsibilities
 Monitor Serum uric acid.
 Encourage patient to maintain a high fluid intake
(3000ml/day).
 Monitor I/O charting, Output should be at-least
2000ml/day.
 Avoid Alcohol.
 Avoid high purine foods like meats and sweet breads.
 Encourage for low purine foods like peanut butter, egg,
fruits and vegetables, Potatoes, rice and pasta.

46. Urologicals
 Medicines used for lower urinary tract symptoms
 Alpha blockers- Flomaxtra (Tamsulosin), Xatral SR
(Alfuzosin), Minipress (Prazosin)
 5 alpha reductase inhibitors- Finasteride (Proscar),
Dutasteride (Avodart)
 Anti-cholinergics-Ditropan (Oxybutynin), Detrusitol
(Tolterodine), Vesicare (Solifenacin)

47. Urologicals

48. Alpha blockers
 These drugs work by relaxing the muscle at the bladder neck
thereby improving the flow of urine.
 Uses-Benign prostatic hypertrophy.
 Contraindications-Hypersensitivity to tamsulosin; in
conjunction with another alpha1A-adrenergic blocking agent;
lactation, pediatric patients.
 Side effects include dizziness, postural hypotension,
headache and retrograde ejaculation.
 Dosage-Adult: PO 0.4 mg q.d. 30 min after a meal, may
increase up to 0.8 mg q.d.

49. 5 alpha reductase inhibitors-
 These drugs inhibit the conversion of testosterone to
dihydrotestosterone, the most potent androgen in the prostate
gland. This causes a “shrinkage” in the size of the prostate gland
thus helping to improve lower urinary tract symptoms. These
drugs take some months to work and the urinary symptoms do
not improve straight away.
 Uses-Benign prostatic hypertrophy, male pattern hair loss
(androgenetic alopecia).
 Dosage- Benign Prostatic Hypertrophy Adult: PO 5 mg/d
and Male Pattern Hair Loss Adult: PO 1 mg q.d.
 Contraindications-Hypersensitivity
 Side effects include loss of libido, impotence, and a reduction in
the volume of the ejaculate.

50. Anti-Cholinergics
 These drugs act to inhibit bladder contractions and increase
bladder capacity.
 Uses-Neurogenic bladder, BPH, Bladder infections, Enuresis
 Contraindications-Hypersensitivity, narrow angle glaucoma,
myasthenia gravis, partial or complete GI obstruction, gastric
retention, paralytic ileus, megacolon, severe colitis, GU
obstruction, urinary retention, unstable cardiovascular status.
 Dosage- 5mg b.d.
 Side effects include dry mouth, constipation, blurred vision,
and tachycardia.

51. Nursing Responsibilities
 Monitor for signs of orthostatic hypotension; take BP lying
down, then upon standing.
 Make position changes slowly to minimize orthostatic
hypotension.
 Keep physician informed of expected responses to drug therapy
(e.g., effect on urinary frequency, urgency, urge incontinence,
nocturia, completeness of bladder emptying).

52. Anti-infectives
 Used to prevent or treat urinary tract infections.
 Methenamine -e.g.Methenamine mandelate andMethenamine
hippurate
 Nitrofurans –e.g.Nitrofurantoin
 Quinoline derivative- e.g. Norfloxacin , Ciprofloxacin

53. Methenamine
 Actions-Tertiary amine liberates formaldehyde in an acid
medium.
 Uses-Prophylactic treatment of recurrent urinary tract
infections (UTIs). Also long-term prophylaxis when residual
urine is present (e.g., neurogenic bladder).
 Dosage- 1g b d
 Contraindications-Renal insufficiency, liver disease, gout,
severe dehydration
 Adverse Effects -Nausea, vomiting, diarrhea, abdominal
cramps, anorexia, Bladder irritation, dysuria, frequency,
albuminuria and hematuria.

54. Nitrofurans
 Actions-Synthetic nitrofuran derivative presumed to act by
interfering with several bacterial enzyme systems. Highly
soluble in urine and reportedly most active in acid urine.
Antimicrobial concentrations in urine exceed those in blood.
 Uses-Pyelonephritis, pyelitis, and cystitis caused by susceptible
organisms.
 Dosage- 50-100mg qid
 Contraindications-Anuria, oliguria, significant impairment of
kidney function (creatinine clearance <40 mL/min); G6PD
deficiency; infants <3 mo. Safety during pregnancy (category
B), pregnancy at term, or lactation is not established
 Adverse effects- Headache, Nausea, Anorexia, Arthralgia,
Pruritis and tooth staining.

55. Quinoline derivatives
 Actions-Inhibits DNA-gyrase, an enzyme necessary for
bacterial DNA replication and some aspects of transcription,
repair, recombination, and transposition.
 Uses-UTIs, lower respiratory tract infections, skin and skin
structure infections, bone and joint infections, GI infection
 Contraindications-Known hypersensitivity to ciprofloxacin or
other quinolones and syphilis
 Dosage- Adult: PO 500–750 mg q12h IV 200–400 mg q12h,
infused over 60 min
 Side-effects- Nausea, vomiting, diarrhea, cramps, Transient
increase in eosinophilia count, Headache, vertigo, malaise,
peripheral neuropathy, seizures (especially with rapid IV
infusion), Pruritis, tendon pain and inflammation.

56. Nursing Responsibilities
 Monitor urine pH; value of 5.5 or less is required for optimum
drug action.
 Monitor I&O charting
 Immediately report tendon inflammation or pain. Drug should
be discontinued.
 Report sudden, unexplained joint pain.
 Restrict caffeine due to the following effects (e.g., nervousness,
insomnia, anxiety, tachycardia).

57. Spermicides
 Spermicide is an agent that kills spermatozoa (sperm).
Spermicide causes the sperm cell membrane to rupture, so the
sperm is unable to fertilize the egg. Creams, jellies, foams etc.,
containing chemical spermicides are used as contraceptives.
 NONOXYNOL-9
 Actions-Nonionic surfactant spermicidal incorporated into
foams, gels, jelly, or suppositories.
 Therapeutic Effects-Applied over the cervix, blocks entrance
to uterus by sperm, traps and absorbs seminal fluid, then
releases the immediately available spermicide. Immobilizes
sperm by cell membrane disruption.

58.  Uses-As barrier contraceptive alone or in conjunction with a
vaginal diaphragm or with a condom.
 Topical Apply or insert 30–60 min before intercourse.
 Contraindications-Cystocele, prolapsed uterus, sensitivity or
allergy to polyurethane or to nonoxynol-9; vaginitis; history of
TSS; pregnancy; immediately after delivery or abortion; during
menstruation.
 Adverse effects-vaginal irritation and dryness; increase in
vaginal infections

59. Nursing responsibilities
Patient teaching
 Stop using nonoxynol-9 if pregnancy is suspected.
 Report symptoms of vaginal infection to physician: Burning,
inflammation, intense vaginal and vulvar itching, cheesy, curd-
like discharge, painful intercourse, dysuria. Nonoxynol-9
antifungal properties are weaker than its antibacterial potency,
thus vulvovaginal candidiasis frequently occurs.
 Use spermicide before the first and every subsequent act of
intercourse.

60. Bibliography
 Trounce’s Clinical pharmacology for nurses; Ben Greenstein;
Dinah gould; 18th ed;Elsevier publications;pg-161-190
 Mosby’s Nursing Drug reference; Linda Skidmore; Roth;26th
ed;Elsevier publications;pg-33,40,129,1078,2045,97
 http://www.pharmacologyeducation.org/drugs/genitourinary-
system
 https://www.drugs.com/drug-class/genitourinary-tract-
agents.html
 https://patient.info/in/medicine/the-genito-urinary-system-1272
 http://www.mayoclinic.org/diseases-conditions/high-blood-
pressure/in-depth/diuretics/art-20048129
 http://www.robholland.com/Nursing/Drug_Guide/data/monogra
phframes/T062.html