Nephrolithiasis Medication

Updated: Dec 03, 2016
  • Author: Chirag Dave, MD; Chief Editor: Bradley Fields Schwartz, DO, FACS  more...
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Medication

Medication Summary

Please see Cystinuria, Hypercalciuria, Hyperoxaluria, Hyperuricosuria and Gouty Diathesis, Hypocitraturia, and struvite topics for specific information regarding medical therapy for stone disease. The medications listed below include those used in the emergency department (ED) and in outpatient management of renal (ureteral) colic, as well as selected antibiotics

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Analgesics, Narcotic

Class Summary

Narcotic analgesics act at the central nervous system (CNS) mu receptors and are the standard of care for treatment of renal colic. They are inexpensive and proven effective. Disadvantages include sedation, respiratory depression, smooth muscle spasm, and potential for abuse and addiction.

Butorphanol

Butorphanol is a mixed agonist-antagonist narcotic with central analgesic effects for moderately severe to severe pain. It causes less smooth muscle spasm and respiratory depression than morphine or meperidine. Weigh these advantages against the increased cost of butorphanol.

Morphine sulfate (Kadian, MS Contin, Infumorph 200, Infumorph 500)

Morphine is the principal opium alkaloid product. It is the drug of choice for parenteral use in the immediate management of pain due to renal (ureteral) colic.

Oxycodone and acetaminophen (Percocet, Endocet, Roxicet, Xartemis XR, Primlev)

Oxycodone-acetaminophen is a drug combination indicated for oral relief of moderate to severe pain. It is employed in medical expulsive therapy (MET).

Hydrocodone and acetaminophen (Vicodin, Vicodin ES, Lortab, Norco, Zamicet)

Hydrocodone is also combined with acetaminophen. This drug combination is indicated for oral relief of moderate to severe pain.

Meperidine (Demerol)

Meperidine is a narcotic analgesic with multiple actions similar to those of morphine. It may produce less constipation, smooth muscle spasm, and depression of cough reflex than similar analgesic doses of morphine.

Nalbuphine

Nalbuphine is a synthetic opioid agonist-antagonist potent analgesic. It stimulates kappa opioid receptor in the CNS, which causes inhibition of ascending pain pathways. It is indicated for the relief of moderate to severe pain.

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Analgesics, Miscellaneous

Class Summary

Analgesics such as acetaminophen can be used to provide relief of mild to moderate pain.

Acetaminophen

Acetaminophen is a nonopioid analgesic that is effective in relieving mild to moderate pain; however, it has no peripheral anti-inflammatory effects but can be used in pregnancy.

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Nonsteroidal anti-inflammatory drugs

Class Summary

Nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit pain and inflammatory reactions by decreasing activity of cyclooxygenase, which is responsible for prostaglandin synthesis. Both properties are beneficial in the management of renal (ureteral) colic.

These agents are at least as effective as narcotic analgesics in numerous randomized controlled trials. NSAIDs cause less nausea and less sedation than narcotic analgesics, do not cause respiratory depression, and have no abuse potential. Their principal disadvantage is cost. Potential adverse effects on renal function, gastrointestinal (GI) mucosa, and platelet aggregation do not appear clinically important when they are used for short-term pain relief.

Ketorolac

Ketorolac inhibits prostaglandin synthesis by decreasing the activity of COX, which results in decreased formation of prostaglandin precursors. Its onset of action is evident within 10 min.

Ketorolac intranasal (Sprix)

Intranasal ketorolac inhibits cyclooxygenase, an early component of the arachidonic acid cascade, resulting in reduced synthesis of prostaglandins, thromboxanes, and prostacyclin. It elicits anti-inflammatory, analgesic, and antipyretic effects. It is indicated for short-term (up to 5 d) management of moderate to moderately severe pain. Bioavailability of a 31.5-mg intranasal dose (2 sprays) is approximately 60% of a 30-mg intramuscular (IM) dose. The intranasal spray delivers 15.75 mg per 100-µL spray; each 1.7-g bottle contains 8 sprays.

Ibuprofen (Motrin, Advil, Addaprin, Caldolor, Dyspel, Genpril)

Ibuprofen is an oral NSAID. It has antipyretic, analgesic, and anti-inflammatory properties and is used for outpatient management.

Celecoxib (Celebrex)

Celecoxib primarily inhibits COX-2. COX-2 is considered an inducible isoenzyme, induced during pain and inflammatory stimuli. Inhibition of COX-1 may contribute to NSAID GI toxicity. At therapeutic concentrations, COX-1 isoenzyme is not inhibited; thus, GI toxicity may be decreased. Seek the lowest dose of celecoxib for each patient. It is extensively metabolized in liver primarily via cytochrome P450 2C9.

Although increased cost can be a negative factor, the incidence of costly and potentially fatal GI bleeds is clearly less with COX-2 inhibitors than with traditional NSAIDs. Ongoing analysis of cost avoidance of GI bleeds will further define the populations that will find COX-2 inhibitors the most beneficial.

Meloxicam (Mobic, Vivlodex)

Meloxicam decreases COX activity, and this, in turn, inhibits prostaglandin synthesis. These effects decrease the formation of inflammatory mediators.

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Corticosteroids

Class Summary

These are strong anti-inflammatory agents that reduce ureteral inflammation. They also have profound metabolic and immunosuppressive effects.

Prednisone (Deltasone, Rayos)

Prednisone has been used in MET. Only a short course of prednisone therapy (5-10 d) should be administered.

Prednisolone (Pediapred, Millipred, Veripred 20, Orapred ODT)

In combination with nifedipine or tamsulosin, prednisolone is proven to facilitate spontaneous passage of a ureteral stone in several small prospective studies. Only a short course of therapy (5-10 d) should be administered.

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Calcium Channel Blockers

Class Summary

Calcium channel blockers are smooth-muscle relaxants. In combination with prednisolone, they have facilitated ureteral stone passage in several small prospective studies.

Nifedipine (Nifedical XL, Afeditab CR, Procardia, Procardia XL, Adalat CC)

Nifedipine facilitates the passage of ureteral stones. The extended-release formulation simplifies treatment and encourages compliance. Only short-term therapy (10 d) should be considered for this indication.

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Alpha Blockers, Antihypertensives

Class Summary

Alpha-blockers are smooth-muscle relaxants. They have been shown to facilitate ureteral stone passage.

Tamsulosin (Flomax)

Tamsulosin, an alpha-1 selective blocker, is indicated for the treatment of lower urinary tract symptoms due to prostatic enlargement. An off-label use, as discussed above, is to facilitate passage of ureteral stones. Only short-term therapy (10 d) should be considered for this indication.

Terazosin

Terazosin is indicated for the treatment of hypertension, as well as lower urinary tract symptoms due to prostatic enlargement. An off-label use is to facilitate passage of ureteral stones. Only short-term therapy (10 d) should be considered for this indication.

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Xanthine Oxidase Inhibitors

Class Summary

Uricosuric agents help prevent nephropathy. They also help prevent recurrent calcium oxalate calculi.

Allopurinol (Zyloprim, Aloprim)

Allopurinol inhibits xanthine oxidase, the enzyme that synthesizes uric acid from hypoxanthine. It reduces the synthesis of uric acid without disrupting the biosynthesis of vital purines.

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Alkalinizing Agents, Oral

Class Summary

Oral alkalinizing agents are used for the treatment of metabolic acidosis. They are also employed when long-term maintenance of alkaline urine is desirable.

Potassium citrate (Urocit K)

Potassium citrate is absorbed and metabolized to potassium bicarbonate, thus acting as a systemic alkalizer. Its effects are essentially those of chlorides before absorption and those of bicarbonates subsequently. Oxidation is virtually complete so that < 5% of the potassium citrate is excreted in the urine unchanged. It is highly concentrated and, when administered after meals and before bedtime, allows maintenance of an alkaline urinary pH at all times, usually without necessity of 2 AM dose. In the recommended dosage, it alkalinizes urine without producing systemic alkalosis.

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Antiemetics

Class Summary

Patients with acute renal colic frequently experience intense nausea and/or vomiting. Effective pain control often is accompanied by resolution of nausea and vomiting, but some patients may require antiemetics in addition to analgesics. Various antiemetic medications are used, including phenothiazines and butyrophenones.

Metoclopramide (Reglan)

Metoclopramide is the only antiemetic that has been studied specifically in treatment of renal colic. In 2 small double-blinded studies, it provided relief of nausea and pain relief equal to that of narcotic analgesics. Metoclopramide's antiemetic effect is due to blockade of dopaminergic receptors in chemoreceptor trigger zone in CNS. Metoclopramide does not possess antipsychotic or tranquilizing activity and is less sedating than other central dopamine antagonists. Onset of action is 1-3 min after intravenous (IV) injection and 10-15 min after IM injection.

Prochlorperazine (Compazine, Compro)

Prochlorperazine may relieve nausea and vomiting by blocking postsynaptic mesolimbic dopamine receptors through its anticholinergic effects and depressing the reticular activating system. 

Promethazine (Phenadoz, Phenergan)

Promethazine is a phenothiazine derivative that possesses antihistaminic, sedative, antimotion sickness, antiemetic, and anticholinergic effects.

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Antibiotics

Class Summary

Infected hydronephrosis mandates IV antibiotic therapy in addition to urgent drainage via percutaneous nephrostomy or urethral stent placement. Aerobic gram-negative enteric organisms, including Escherichia coli and Klebsiella, Proteus, Enterobacter, and Citrobacter species, are typical pathogens. Enterococcal infection occasionally is seen in patients recently on antibiotics. Candida albicans sometimes is responsible in diabetic or immunosuppressed patients. Initial empiric antibiotic therapy should cover common bacterial pathogens.

Ampicillin

Ampicillin is a beta-lactam aminopenicillin antibiotic. Non–penicillinase-producing staphylococci and most streptococci are susceptible. Ampicillin is effective against E coli and Proteus and Enterococcus species, but most Klebsiella, Serratia, Acinetobacter, indole-positive Proteus, and Pseudomonas species and Bacteroides fragilis are resistant. Ampicillin is usually combined with gentamicin.

Gentamicin

Gentamicin is an aminoglycoside antibiotic, which is active against Staphylococcus aureus and Enterobacteriaceae organisms including E coli and Proteus, Klebsiella, Serratia, Enterobacter, and Citrobacter species. Pseudomonas aeruginosa is usually sensitive, although its sensitivity varies somewhat. When used in combination with ampicillin, gentamicin also effective against Enterococcus faecalis.

Ticarcillin and clavulanic acid (Timentin)

Ticarcillin is an extended-spectrum penicillin, beta-lactam antibiotic. Clavulanic acid is a beta-lactamase inhibitor that, in combination with ticarcillin, extends the spectrum of ticarcillin to include many beta-lactamase–producing bacteria. Ticarcillin-clavulanate is excreted via the urinary tract.

This combination is active against most staphylococci and streptococci and gram-negative organisms including E coli, Morganella morganii, Proteus mirabilis, Proteus vulgaris, Neisseria gonorrhoeae, and Pseudomonas and Providencia species; the anaerobic spectrum includes Peptococcus and Peptostreptococcus species, Clostridium perfringens, Clostridium tetani, and Bacteroides species, including many strains of B fragilis. It is not effective against Enterococcus species or methicillin-resistant staphylococci.

Ciprofloxacin (Cipro)

Ciprofloxacin is a reasonable alternative for treating infected hydronephrosis in penicillin-allergic patients. Fluoroquinolones are active against aerobic gram-negative organisms and generally effective against aerobic gram-positive organisms, though some resistance has been noted in S aureus and Streptococcus pneumoniae. Ciprofloxacin is not effective against anaerobes. It is variably effective against E faecalis, though ampicillin and gentamicin are likely to be more effective.

Levofloxacin (Levaquin)

Levofloxacin is a reasonable alternative for treating infected hydronephrosis in penicillin-allergic patients. Fluoroquinolones are active against aerobic gram-negative organisms and generally effective against aerobic gram-positive organisms, though some resistance has been noted in S aureus and S pneumoniae. Levofloxacin is not effective against anaerobes. It is variably effective against E faecalis, though ampicillin and gentamicin are likely to be more effective.

Ofloxacin

Ofloxacin is a reasonable alternative for treating infected hydronephrosis in penicillin-allergic patients. It is active against aerobic gram-negative organisms and generally effective against aerobic gram-positive organisms, though some resistance has been noted in S aureus and S pneumoniae. It is not effective against anaerobes. It is variably effective against E faecalis, though ampicillin and gentamicin are likely to be more effective.

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