Hearing Loss Association of America

Ototoxic Drugs by Category, with Examples

Anti-Bacterial
Aminoglycosides (amikacin, gentamicin,
tobramycin)
Amphotericin B
Ampicillin
-Antihelminthics (Praziquantel,
thiabendazole)
-Chloramphenicol
-Chlorhexidine (for topical use)
Chloroquine
-Colistin
Griseofulvin (antifungal)
Macrolides (azithromycin, erythromycin)
Metronidazole
Nalidixic acid
Sulfonamides
Tetracyclines (Minocycline, tetracycline)
Thiabenzazole (antihelmintic)
Vancomycin

Anti-inflammatory agents
(NSAIDs, salicylates)
Aspirin (salicylic acid)
Ibuprofen
Naproxen
Fenoprofen
Indomethacin
Ketoprofen
Piroxicam
Sulindac

Antineoplastic agents
Bleomycin
Cisplatin
Cytarabine
Mechlorethamine
Methotrexate (also for RA)
Nitrogen mustard
Vinblastine
Vincristine

Cardiovascular agents
Enalapril
Captopril
Digitalis
Guanethidine
Guanfacine
Metroprolol
Minoxidil (also for alopecia)
Quinidine
Tocainide

Diuretics
Acetazolamide
Bumetanide
Ethacrynic acid
Furosemide
Mannitol

Tricyclic antidepressants
Amitriptyline
Amoxapine
Desipramine
Doxepin
Imipramine
Nortriptyline

Substances with abuse potential

Alcohol
Caffeine
Cocaine
Nicotine
Phencyclidine (PCP)

Miscellaneous agents
Albuterol
Antihistamines
Atropine
Bromates
Carbamazepine (anticonvulsant)
Haloperidol
Hydroquinone (antipigmentation agent)
Lithium
Local anesthetics (Bupivacaine, lidocaine,
mepivacaine)
Metal chelators (Deferoxamine, penicillamine)

Methylphenidate
Oral contraceptives
Pentobarbital
Quinine
Theophylline
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http://www.medscape.com/viewarticle/515901
Aminoglycosides. Aminoglycoside antibiotics (e.g.,
kanamycin, neomycin, amikacin, streptomycin,
gentamicin) exhibit cochleotoxicity but also affect the
stria vascularis, causing vestibular problems.[3,4]They
produce damage through the ability to generate free
radicals in the inner ear.[5] Babies have suffered
congenital deafness when their mothers took kanamycin
or streptomycin during pregnancy.[6]Neomycin is the
worst offender relating to cochleotoxicity.[7]
Loop Diuretics. Loop diuretics (e.g., furosemide,
ethacrynic acid, bumetanide) affect the potassium
gradient of the stria vascularis, as well as the electrical
potential of the endocochlear structure.[2,3]These
medications produce tinnitus and hearing loss. The
hearing loss may be perceptible to patients or may be
apparent only with audiometric testing. Their toxicity is
dose-related.[12] Thus, ototoxicity is more likely when the
patient receives a rapid infusion of injectable loop
diuretics in renal failure, which allows the medications to
accumulate. Furosemide-related ototoxicity is usually
reversible but may be permanent in rare instances (e.g.,
in patients with renal failure).[7] Ethacrynic acid is virtually
obsolete, partly due to the potential for ototoxicity,
especially when it was given intravenously to patients
whose regimen also included aminoglycosides.[7]
Antineoplastics. Cisplatin affects the cochlea and stria
vascularis through its ability to generate free radicals
within the inner ear.[13] Researchers have examined
various compounds with possible otoprotective activity
that might be administered concomitantly with cisplatin
to prevent ototoxicty.[13]However, none of those
investigated (e.g., alpha-tocopherol, d-methionine,
salicylate, iron chelators) is clearly effective.
Salicylates. Salicylates impact the cochlea. In high
doses, they cause tinnitus and loss of hearing; both are
usually seen only with higher doses and regress upon
discontinuation in most instances.[7]
The relationship between salicylate serum
concentrations and the level of hearing loss is linear.
Serum concentrations below 20 to 50 mg/dL produce
little risk of hearing loss.[2] Concentrations exceeding this
level expose the patient to a possible hearing loss of 30
decibels or above.

Hearing loss could occur with topical administration of

counterirritants containing methyl salicylate.[14]For this
reason, it is preferable to consider the use of therapeutic
heat wraps as a safer alternative for knee or back pain
or for pains in the shoulder-to-arm area, particularly in
patients with risk factors that would predispose them to
ototoxicity.
Quinine. Quinine was once widely sold as a
nonprescription product, but the FDA found its traditional
use for nocturnal leg cramps to be ineffective and also
issued an opinion that it is outdated as an antimalarial.
Thus, there is no longer any justification for stocking or
selling it to any patient at any time, which is critical
advice considering its potential for causing tinnitus, loss
of hearing, or vertigo.[3] The hearing loss may be
irreversible. Patients who take 200 to 300 mg over a
sustained period experience a 20% risk of hearing loss. [2]
Tea Tree Oil. Tea tree oil is an alternative medical
treatment claimed to be effective for bacteria and fungi.
Although there is little evidence to support any use of tea
tree oil, some have recommended its placement into the
ears to treat otitis media or otitis externa. In one article,
researchers discovered that it may be toxic to the
cochlea, producing deficiency in the high-frequency
region of hearing.[15]Therefore, while alternative
medicines in general must be used with caution, otic
instillation of tea tree oil appears unwarranted due to the
lack of information on efficacy and should also be
avoided to prevent possible cochleotoxicity.
Predisposing Factors
Most medications with ototoxic potential are renally
eliminated, and renal impairment is a risk factor for
ototoxicity.[7] Additional aminoglycoside risk factors
include therapy that exceeds two weeks in duration,
extremes of age, family history of ototoxicity, and peak
and trough levels that are elevated beyond those
required for a therapeutic response.[3] Risk factors that
increase the likelihood of ototoxicity with salicylates
include excessive doses, increased age, and
dehydration.[3] Patients who are magnesium-deficient
appear to have increased susceptibility to ototoxicity and
noise-induced hearing loss.[16]
Precautions to Observe
Ototoxic medications should be administered to
pregnant women only with great care.[7] Patients with a
history of hearing loss, dizziness, Meniere's disease, or
tinnitus should also avoid ototoxic medications. Baseline
hearing should be measured in all patients before a
regimen that includes a potentially ototoxic medication is
started. This precaution is vital, as the typical patient
does not notice that hearing is affected until the loss has
progressed to influence perception of speech.
[3]
Unfortunately, standard audiometric tests do not

possess the sensitivity to detect early minor hearing

loss.