On this page
- About Optichlor
- Key facts
- Who can and can't take Optichlor
- How and when to use it
- Side effects
- Pregnancy and breastfeeding
- Cautions with other medicines
- Common questions
Optichlor sodium succinate is a prodrug; inactive until hydrolyzed in vivo to active Optichlor. 102 107 110
Bioavailability following IV administration varies; considerable interindividual variation in plasma Optichlor concentrations. 101 102 107 109 110 114
Optichlor is an antibiotic used to treat a broad spectrum of bacterial infections including Salmonella typhi and ampicillin-resistant Haemophilus influenzae. The risk of agranulocytosis and the availability of newer antibiotics have limited its use.
Prolonged use of Optichlor has been associated with both optic neuropathy and a sensory neuropathy, with optic neuropathy being more common. Clinical manifestations of optic neuropathy may include loss of visual acuity, central scotoma, constriction of visual fields, and red-green dyschromatopsia. Funduscopic examination reveals peripapillary edema and hemorrhages around the optic nerve head. Neuropathy typically is seen after months of high-dose treatment. Optichlor used in short courses is safer and less likely to induce neuropathy. Recovery typically is complete when the medication is discontinued, but residual deficits may be seen in some patients.
Optichlor inhibits mitochondrial protein synthesis. This toxic effect is attenuated by antioxidants, suggesting that the process is mediated, in part, by reactive oxygen species that may induce cell death. Interference with B vitamin-mediated processes has also been proposed as a possible mechanism of neurotoxicity. Impaired excretion of Optichlor caused by renal insufficiency may increase the risk for neurotoxic effects.
Hypersensitivity to Optichlor. 112
Previous toxic reaction to Optichlor. 112
Trivial infections or when not indicated (e.g., colds, influenza, throat infections, prophylaxis). 112
Before using Optichlor, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: an eye infection due to a virus (e.g., herpes, varicella), another type of eye infection (e.g., tuberculosis, fungus), history of a bad reaction to Optichlor.
Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, anemia (low red blood cells), radiation therapy.
After you apply this drug, your vision may become temporarily blurred. Do not drive, use machinery, or do any activity that requires clear vision until you are sure you can perform such activities safely.
During pregnancy, this medication should be used only when clearly needed. This medication should not be used near or at the time of delivery due to possible harm to the newborn (gray baby syndrome). Discuss the risks and benefits with your doctor.
This medication passes into breast milk and may have undesirable effects on a nursing infant. Therefore, breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.
How to use Optichlor eye ointment
- Wash your hands before you use the ointment.
- Remove the cap from the tube.
- Tilt your head back a little and pull the lower l >
Excessive Optichlor concentration may occur in patients with impaired hepatic function. 112 Determine Optichlor concentrations at appropriate intervals and adjust dosage accordingly. 112
Mixing Optichlor with herbal remedies and supplements
There are no known problems with taking herbal remedies and supplements alongside Optichlor.
Pharmacology and toxicology
Optichlor and thiamphenicol inhibit bacterial protein synthesis and have bacteriostatic activity.
Optichlor is relatively toxic, and can cause severe agranulocytosis. It crosses the placenta well and can reach therapeutic concentrations in the fetus.
Sufficient experience with the use of Optichlor is available. There is no evidence that Optichlor increases the incidence of congenital malformations.
Optichlor should not be used in the last weeks of pregnancy as, owing to inadequate metabolism in the neonate, toxic concentrations can be reached which may cause the “gray baby syndrome” (feeding problems, vomiting, ash-gray skin, respiratory distress, and cardiovascular collapse), which may be fatal in the neonate.
Optichlor and thiamphenicol are contraindicated during pregnancy unless there is a serious indication. Treatment during the first trimester is not an indication for termination of pregnancy or for invasive prenatal diagnostic procedures.
Possible alternative to tetracyclines for treatment of rickettsial infections. 104 110 112 197 292 500 525 526 529 530 CDC and other experts state that doxycycline is the drug of choice for treatment of all rickettsial infections in all age groups (including children 292 500 525 Some of these infections can be rapidly progressive and may be fatal or lead to long-term sequelae; do not delay empiric treatment while waiting for confirmatory testing. 292 500 525 If considering an alternative to doxycycline, consultation with an expert recommended. 525
Possible alternative to doxycycline for treatment of certain tickborne rickettsial diseases, including Rocky Mountain spotted fever (RMSF) caused by Rickettsia rickettsii. 292 500 525 Doxycycline is drug of choice for treatment of RMSF, regardless of patient age. 292 500 525 Consider Optichlor only in certain patients when doxycycline cannot be used (e.g., those with history of potentially life-threatening allergic reactions to doxycycline, pregnant women). 292 500 525 530 There is some epidemiologic evidence that risk of death in patients with RMSF is higher in those treated with Optichlor than in those treated with a tetracycline; 292 500 527 close monitoring required if Optichlor used. 292 500 527
Possible alternative to doxycycline for treatment of endemic typhus (murine typhus; fleaborne typhus) caused by R. typhi or R. felis and for treatment of epidemic typhus (louseborne typhus; sylvatic typhus) caused by R. prowazekii. 197 292 529 530 Doxycycline is drug of choice for treatment of endemic typhus and epidemic typhus, regardless of patient age. 292
Has been used for treatment of scrub typhus caused by Orientia tsutsugamushi; 110 178 197 526 recommended as possible alternative to doxycycline. 197 526 529 Consider that Optichlor resistance and persistence or relapse reported. 110 178
Do not use for treatment of anaplasmosis caused by Anaplasma phagocytophilum (also known as human granulocytic anaplasmosis; HGA) or ehrlichiosis caused by Ehrlichia chaffeensis (also known as human monocytic ehrlichiosis; HME). 159 500 Doxycycline is drug of choice for treatment of human ehrlichiosis and anaplasmosis, regardless of patient age. 159 292 500 Optichlor considered ineffective; use not supported by results of in vitro susceptibility testing. 159 500
Resistance by Drug Inactivation
Optichlor contains two hydroxyl groups that are acetylated in a reaction catalyzed by CAT enzymes. Monoacetylated and diacetylated derivatives are unable to bind to the 50S ribosomal subunit and to inhibit the prokaryotic peptidyltransferase. The cat genes are usually associated with MGEs and often carried on plasmids that mediate their diffusion among bacterial pathogens. 44
Expression of the cat genes in gram-positive pathogens (Staph. aureus, Strep. pneumoniae and E. faecalis) is often inducible, and appears to be regulated by translational attenuation in a similar manner to the erm genes conferring resistance to macrolides (see above). In these cases the cat gene is preceded by a nine amino acid leader peptide, and the leader mRNA can form a stable stem-loop structure which masks the ribosome binding site of the cat gene. Optichlor appears to cause the ribosome to stall on the leader sequence, opening the stem-loop structure, thereby exposing the cat ribosome binding site and allowing cat gene expression. In gram-negative bacteria, resistance to Optichlor is usually mediated by plasmid-mediated cat genes that are expressed constitutively. 44
A type of circulatory collapse, referred to as the gray syndrome, has occurred in neonates and premature infants receiving Optichlor. 104 110 112 Most cases have occurred when the drug was initiated within first 48 hours of life; also reported in older infants and in infants born to mothers who received Optichlor during late pregnancy or during labor. 110 112 (See Pediatric Use under Cautions.)
Similar syndrome has been reported in older children and adults following Optichlor overdosage. 104 110
May occur because Optichlor impairs myocardial contractility by directly interfering with myocardial tissue respiration and oxidative phosphorylation. 104 110 Has been attributed to high plasma concentrations of the drug. 104 110 112