N01BB04 - Prilocaine |
Not porphyrinogenic |
NP |
Rationale
Used uneventfully in 105 patients with latent or active acute porphyria. By clinical criteria the local anaesthetic prilocaine is not porphyrinogenic.
Chemical description
Prilocaine hydrochloride is a local anaesthetic of the amide type.
Therapeutic characteristics
Local anaesthetic.
Hepatic exposure
Volume required to reach uM concentrations when injected intravenously: approximately 2 ml (of prilocaine 30 mg/ml).
Metabolism and pharmacokinetics
Prilocaine hydrochloride is metabolized principally in the liver. Some metabolism of prilocaine may also occur in the kidneys. Prilocaine is excreted in urine as various metabolites and less than 1% as unchanged drug. Not been found to be an inducer or irreversible inhibitor of drug metabolizing cytochrome P450 species (Rendic, 2002).
Personal communication
Thunell, S., study to be published: 105 patients exposed without porphyric adverse reaction reported. Andersson: Reports to have frequently used it in infiltrations without illeffects.
IPNet drug reports
Uneventful use reported in 6 patients with acute porphyria.
Similar drugs
References
| # | Citation details | PubMed ID |
|---|---|---|
| 1. | Regional anesthesia as anesthetic technique of choice in acute hepatic porphyria.
Böhrer H, Schmidt H. J Clin Anesth. 1992; 4(3):259.
|
1610588 |
| 2. | Study of anaesthetic agents for their ability to elicit porphyrin biosynthesis in chick embryo liver.
de Verneuil H, Deybach JC, et al. Biochem Pharmacol. 1983 Mar; 32(6):1011-8.
|
6838647 |
| 3. | Effect of certain anaesthetic agents on the activity of rat hepatic delta-aminolaevulinate synthase.
Parikh RK, Moore MR. Br J Anaesth. 1978 Nov; 50(11):1099-103.
|
718778 |
| 4. | Summary of information on human CYP enzymes: human P450 metabolism data.
Rendic S. Drug Metab Rev. 2002; 34(1-2):83-448.
|
11996015 |
| Drug reference publications | ||
| 5. | Sweetman SC, editor. Martindale: The complete drug reference. Prilocaine Hydrochloride. Pharmaceutical Press 2009.
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|
| 6. | Prilocaine Hydrochloride.
McEvoy GK, editor. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (March 2009).
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| Other sources | ||
| 7. | Thunell, S. Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published).
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Tradenames
Citanest · Prilotekal 
Citanest · Tachipri 
Takipril Hiperbarica 
Prilotekal 
Prilotekal 
Prilocain 
Citanest · Prilocaine · Prilotekal 
Takipril 
Citanest · Prilotekal · Takipril · Xylonest 
Takipril 
Prilotekal 
Prestige · Prilotekal 
Citanest 
Citanest Octapressin · Takipril 
4% Citanest 
Citanest · Tachipri 
Takipril 
Takipril · Takipril Hiperbarica 
Takiprin