Citrates

Drug class: Antineoplastic Agents

Usage of Citrates

Preparations containing sodium citrate and citric acid are especially useful when administration of potassium salts is undesirable or contraindicated, while those containing potassium citrate and citric acid are used when administration of sodium salts is undesirable or contraindicated.

Alkalinization of Urine

Citrates are used for alkalinization of urine (as alternatives to sodium bicarbonate) in conditions where long-term maintenance of an alkaline urine is desirable (e.g., management of uric acid and cystine calculi of the urinary tract).

Chronic Metabolic Acidosis

Citrates are used for management of chronic metabolic acidosis associated with conditions such as chronic renal insufficiency or renal tubular acidosis.

Adjuvant in Gout Therapy

Citrates are used as adjuvants to uricosuric agents in gout therapy.

Prevention of Milk Curdling

Sodium citrate has been used to alter cow’s milk so that large hard curds are not formed in the stomach of feeding infants† [off-label].

Gastric Acid Neutralization

Some citrate salts (e.g., sodium citrate and citric acid) also used for buffering and neutralizing gastric hydrochloric acid.

Compounding Uses

Sodium citrate and citric acid may be used as a buffer to maintain an approximate pH in various extemporaneous formulations. (See Compatibility under Stability.)

Relate drugs

How to use Citrates

General

  • Selection of a specific preparation may in part be determined by potassium and sodium content.
  • Unlike sodium bicarbonate solution, citrate solutions generally are considered highly palatable and pleasant tasting, and may be particularly useful as alkalinizing agents in patients who do not tolerate the taste of sodium bicarbonate oral solution.

    • Administration

    Oral Administration

    Dilute oral citrate solutions with adequate amounts of water prior to administration to minimize the risk of GI complications, and follow with additional water after administration; enhance palatability by chilling the solution before administration.

    Reconstitute contents of single-dose packets containing potassium citrate and citric acid for oral solution with cool water or juice prior to administration; give additional water or juice after administration.

    Administer oral citrate solutions after meals to avoid the saline laxative effect of the drugs as well as upset stomach.

    Shake oral solutions well before use, unless otherwise directed.

    Reconstitution

    Reconstitute contents of single-dose packets containing potassium citrate and citric acid for oral solution with at least 180 mL of cool water or juice prior to administration.

    Dosage

    Pediatric Patients

    General Pediatric Dosage Potassium Citrate and Citric Acid Oral

    Usually, 5–15 mL of solution, diluted with 1/2 glass of water, after meals and at bedtime.

    Do not use single-dose packets of potassium citrate and citric acid for oral solution in pediatric patients, since dosage for these patients can be more easily regulated with the commercially available oral solution. Individualize dosage according to the patient’s tolerance and response.

    Sodium Citrate and Citric Acid Oral

    Children ≥2 years of age: Usually, 5–15 mL of solution, diluted in 30–90 mL of water, after meals and at bedtime; individualize dosage according to patient’s tolerance and response. Consult a clinician for use in children <2 years of age.

    Tricitrates Oral

    Usually, 5–15 mL 4 times daily, after meals and at bedtime; individualize dosage according to patient’s tolerance and response.

    Prevention of Milk Curdling Sodium Citrate Oral

    Prevention of the formation of large curds in the stomach of feeding infants: Add 100 mg of sodium citrate to each 30 mL of cow’s milk.

    Adults

    General Adult Dosage Potassium Citrate and Citric Acid Oral

    Usually, 15–30 mL of solution, diluted with 1 glass of water, after meals and at bedtime. The usual dosage of potassium citrate and citric acid for oral solution is one single-dose packet (containing 3300 mg of potassium citrate monohydrate and 1002 mg of citric acid monohydrate), reconstituted as directed 4 times daily, after meals and at bedtime. Individualize dosage according to patient’s tolerance and response.

    Sodium Citrate Oral

    Usually, 1–2 g every 2–4 hours as necessary for alkalinization effect.

    Sodium Citrate and Citric Acid Oral

    Usually, 10–30 mL of solution, diluted in 30–90 mL of water, after meals and at bedtime. Individualize dosage according to patient’s tolerance and response.

    Tricitrates Oral

    Usually, 15–30 mL of solution diluted in water 4 times daily, after meals and at bedtime. Individualize dosage according to the patient’s tolerance and response.

    Gastric Acid Neutralization Sodium Citrate and Citric Acid Oral

    15 mL of solution, diluted in 15 mL of water, taken as a single dose.

    Warnings

    Contraindications

  • Potassium citrate and citric acid (oral solution and for oral solution [Cytra-K Crystals]): Manufacturer states that preparation is contraindicated in severe renal impairment with oliguria or azotemia, untreated Addison’s disease, adynamia episodica hereditaria, acute dehydration, heat cramps, anuria, severe myocardial damage, or hyperkalemia (from any cause).
  • Sodium citrate and citric acid oral solution (Bicitra, Cytra-2): Manufacturers state that preparations are contraindicated in patients requiring sodium-restricted diet and those with severe renal impairment.
  • Sodium citrate and citric acid (Oracit): Manufacturer states that preparation is contraindicated in severe renal impairment, oliguria or azotemia, untreated Addison’s disease, adynamia episodica hereditaria, acute dehydration, heat cramp, anuria, severe myocardial damage, and hyperkalemia.
  • Tricitrates oral solution (e.g., Cytra-3): Manufacturer states that preparation is contraindicated in severe renal impairment with oliguria and azotemia, untreated Addison’s disease, and severe myocardial damage.

    • Warnings/Precautions

    Warnings

    Electrolyte and Acid-Base Disturbances

    Potassium-containing formulations: Large doses may cause hyperkalemia and alkalosis, especially in patients with renal impairment. Listlessness, weakness, mental confusion, and tingling of the extremities may be associated with hyperkalemia.

    Sodium-containing formulations: Excessive doses may cause metabolic alkalosis, especially in patients with hypocalcemia or renal impairment. Possible tetany or depression of the heart associated with decreased ionized calcium concentrations may occur with large doses.

    General Precautions

    Concomitant Disease

    Sodium-containing formulations: Use with extreme caution in patients with low urine output (unless patient is closely supervised), CHF, hypertension, renal dysfunction, peripheral or pulmonary edema, or toxemia of pregnancy.

    Potassium-containing formulations: Use with extreme caution in patients in whom excessive potassium may cause deleterious effects.

    Adequate Patient Evaluation and Monitoring

    Evaluate patient’s clinical condition and monitor serum electrolyte concentrations and acid-base balance periodically, especially in patients with renal impairment, to avoid complications.

    Laxative Effects

    Possible saline laxative effects; dilute citrate solution with water and administer after meals to minimize this effect.

    Specific Populations

    Pregnancy

    Potassium citrate: Category A.

    Lactation

    Not known whether potassium citrate is distributed into milk. Because potassium freely distributes into and out of milk, use of potassium citrate by nursing woman with normal plasma potassium concentrations should have no adverse effect on nursing infant; milk potassium concentrations may be increased in hyperkalemic women.

    Renal Impairment

    Use citrates with caution in patients with renal impairment. Monitor serum electrolyte concentrations and acid-base balance to avoid complications (see Warnings/Precautions under Cautions). Manufacturers state that citrates are contraindicated in patients with severe renal impairment (see Contraindications under Cautions).

    Common Adverse Effects

    Generally well tolerated at recommended dosages in patients with normal renal function and urine output. (See Warnings under Cautions.)

    What other drugs will affect Citrates

    Specific Drugs

    Drug

    Interaction

    Comments

    ACE inhibitors

    Potential for hyperkalemia and toxicity with citrate preparations containing potassium

    Amphetamines

    Urinary alkalinization may decrease renal elimination of amphetamines

    Avoid concomitant use, especially in amphetamine overdosage

    Antacids (aluminum-containing)

    Increased GI absorption of aluminum; risk of aluminum toxicity in patients with chronic kidney disease receiving citrates and aluminum-containing drugs

    Avoid concomitant use in patients with chronic kidney disease; sodium bicarbonate may be an alternative if aluminum-containing phosphate binders required

    Cardiac glycosides

    Potential for toxicity

    Chlorpropamide

    Urinary alkalinization may increase renal elimination of chlorpropamide

    Diuretics, potassium-sparing

    Potential for hyperkalemia and toxicity with citrate preparations containing potassium

    Eplerenone

    Potential for hyperkalemia and toxicity with citrate preparations containing potassium

    Lithium

    Urinary alkalinization may increase renal lithium clearance

    Potassium-containing drugs

    Potential for hyperkalemia and toxicity with citrate preparations containing potassium

    Pseudoephedrine

    Urinary alkalinization may decrease elimination of pseudoephedrine

    Pseudoephedrine dosage reduction may be needed

    Quinidine

    Urinary alkalinization may decrease elimination of quinidine

    Monitor ECGs and serum quinidine concentrations if citrate therapy is initiated or discontinued in a patient receiving a stable quinidine dosage

    Salicylates

    Urinary alkalinization may increase renal elimination of salicylates; possible decreased therapeutic and toxic effects of salicylates

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