      Document 0036
 DOCN  DRG0036
 UNIQUE IDENTIFIER        DRG-0211
 NAME OF SUBSTANCE        Levocarnitine [USAN 1996]
 REGISTRY NUMBER          541-15-1
 STANDARD CHEMICAL NAME   1-Propanaminium,
                          3-carboxy-2-hydroxy-N,N,N-trimethyl-,
                          hydroxide, inner salt, (R)- [USAN 1996]
 SYNONYMS                 L-carnitine [CHEMLINE]
 SYNONYMS                 Vitamin BT [Merck Index 1989]
 SYNONYMS                 Cardiogen [Merck Index 1989]
 SYNONYMS                 Carnitene [Merck Index 1989]
 SYNONYMS                 Carnicor [Merck Index 1989]
 SYNONYMS                 Carnitor [USAN 1996]
 SYNONYMS                 Carrier [Merck Index 1989]
 SYNONYMS                 Levocarnil [Merck Index 1989]
 SYNONYMS                 Metina [Merck Index 1989]
 SYNONYMS                 VitaCarn Liquid [Drug Evaluations Annual
                          1995]
 SYNONYMS                 Carnitine (L-Form) [CHEMLINE]
 PROTOCOL ID NUMBERS      NINDS 93 N-30
 SECONDARY SOURCE ID      DRG
 PHARMACOLOGICAL ACTION   MODE OF ACTION: Carrier molecule in the
                          transport of long chain fatty acids across
                          the inner mitochondria, delivering substrate
                          for oxidation and subsequent energy
                          production. Fatty acids are utilized as an
                          energy substrate in all tissues except the
                          brain. The mean distribution half-life for a
                          20 mg/kg IV dose was 0.585 and the mean
                          apparent terminal elimination half-life of
                          total levocarnitine was 19.4 h. Mean renal
                          clearance was about 3.0 L/h; 85% of the dose
                          was excreted as total levocarnitine in 24 h.
                          [PDR 1995] [J Pharm Sci 1995 Apr;84(5)]
 DISEASES STUDIED/TREATED Zidovudine-induced myopathy resulting from
                          carnitine deficiency [NINDS 93 N-30]
 CLASSIFICATION CODE      Antihyperlipoproteinemic [Merck Index 1989]
 OTHER MAJOR USES         Acute and chronic treatment of inborn errors
                          of metabolism that result in carnitine
                          deficiency [PDR 1995]
 SUBSTANCE INTERACTIONS   Levocarnitine can be competitively inhibited
                          by D,L-carnitine; requirements for
                          levocarnitine may be increased in patients
                          receiving valproic acid. [Drug Evaluations
                          Annual 1992] [USP DI 1995]
 ADVERSE EFFECTS          Adverse effects include mild gastrointestinal
                          complaints, including transient nausea and
                          vomiting, abdominal cramps, and diarrhea; and
                          drug-related body odor. [PDR 1995]
 CHEMICAL/PHYSICAL DATA   DRUG DESCRIPTION: Naturally occurring
                          essential cofactor of fatty acid metabolism.
                          Used as a nutritional supplement for
                          treatment of primary or secondary carnitine
                          deficiencies [Drug Evaluations Annual 1992]
 CHEMICAL/PHYSICAL DATA   MOLECULAR FORMULA: C7H15NO3 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MOLECULAR WEIGHT: 161.20 [USAN 1996]
 CHEMICAL/PHYSICAL DATA   MELTING POINT: 196-197 C [PDR 1995]
 CHEMICAL/PHYSICAL DATA   SOLUBILITY: Soluble in water, hot alcohol.
                          Practically insoluble in acetone, ether,
                          benzene [Merck Index 1989]
 CHEMICAL/PHYSICAL DATA   STABILITY: Very hygroscopic solid [Merck
                          Index 1989]
 CHEMICAL/PHYSICAL DATA   PHYSICAL COMMENT: pH: 6.8 (solution); pKa 3.8
                          [PDR 1995]
 CHEMICAL/PHYSICAL DATA   PHYSICAL DESCRIPTION: White powder [PDR 1995]
 SUBSTANCE DELIVERY DATA  DOSAGE FORM: 300 mg tablets; oral solution, 1
                          g/10 ml; 5 ml ampuls (1 g/5 ml) for
                          injection. [PDR 1995]
 SUBSTANCE DELIVERY DATA  MODE OF DELIVERY: Oral; intravenous. [PDR
                          1995]
 SUBSTANCE DELIVERY DATA  STORAGE: Tablets, injections and oral
                          solutions; store at 25 C. Protect ampules
                          from light. [USP DI 1995]
 MANUFACTURERS            Drugs are provided by each participating unit
                          site
 REFERENCES               Mintz M. Carnitine in human immunodeficiency
                          virus type 1 infection/acquired immune
                          deficiency syndrome. J Child Neurol. 1995
                          Nov;10 Suppl 2:S40-4.
 REFERENCES               Famularo G, De Simone C. A new era for
                          carnitine? Immunol Today. 1995
                          May;16(5):211-3.
 REFERENCES               Vitali G, Parente R, Melotti C. Carnitine
                          supplementation in human idiopathic
                          asthenospermia: clincal results. Drugs Exp
                          Clin Res 1995;21(4):157-9.
 REFERENCES               Semino-Mora MC, Leon-Monzon ME, Dalakas MC.
                          Effect of L-carnitine on the
                          zidovudine-induced destruction of human
                          myotubes. Part I: L-carnitine prevents the
                          myotoxicity of AZT in vitro. Lab Invest. 1994
                          Jul;71(1):102-12.
 REFERENCES               Semino-Mora MC, Leon-Monzon ME, Dalakas MC.
                          The effect of L-carnitine on the AZT-induced
                          destruction of human myotubes. Part II:
                          Treatment with L-carnitine improves the
                          AZT-induced changes and prevents further
                          destruction. Lab Invest. 1994
                          Nov;71(5):773-81.
 REFERENCES               De Simone C, Famularo G, Tzantzoglou S,
                          Trinchieri V, Moretti S, Sorice F. Carnitine
                          depletion in peripheral blood mononuclear
                          cells from patients with AIDS: effect of oral
                          L-carnitine. AIDS. 1994 May;8(5):655-60.
 REFERENCES               Dalakas MC, Leon-Monzon ME, Bernardini I,
                          Gahl WA, Jay CA. Zidovudine-induced
                          mitochondrial myopathy is associated with
                          muscle carnitine deficiency and lipid
                          storage. Ann Neurol. 1994 Apr;35(4):482-7.
 REFERENCES               De Simone C, Tzantzoglou S, Famularo G,
                          Moretti S, Paoletti F, Vullo V, Delia S. High
                          dose L-carnitine improves immunologic and
                          metabolic parameters in AIDS patients.
                          Immunopharmacol Immunotoxicol. 1993
                          Jan;15(1):1-12.
 REFERENCES               Grau JM, Casademont J, Pedrol E,
                          Fernandez-Sola J, Cardellach F, Barros N,
                          Urbano-Marquez A. Chronic fatigue syndrome:
                          studies on skeletal muscle. Clin Neuropathol.
                          1992 Nov-Dec;11(6):329-32.
 REFERENCES               De Simone C, Tzantzoglou S, Jirillo E, Marzo
                          A, Vullo V, Martelli EA. L-carnitine
                          deficiency in AIDS patients. AIDS. 1992
                          Feb;6(2):203-5.
 ENTRY MONTH              9405
 LAST REVISION DATE       960424
 

SOURCE: National Library of Medicine, Bethesda, MD.  Distributed by AEGIS.
