Naphazoline

Naphazoline

>>Drug product:

Naphazoline Hydrochloride        Naphcon� Eye Drops
Naphazoline Hydrochloride        Privine�     Nasal Spray

>>Manufacturing company:

Alcon          *Naphcon*
Novartis     *Privine*

>>Ingredients:

>Major active Ingredient:
Naphazoline HCl, USP 0.012% *Naphcon Ophthalmic*
Naphazoline HCl, USP 0.05%    *Privine Nasal*

>Other active Ingredients:
(Preservative) Benzalkonium Chloride 0.01%.
>Inactive Ingredients:
Naphcon Ophthalmic: Boric Acid, Sodium Chloride, Potassium Chloride, Disodium Edetate, Sodium Carbonate and/or Hydrochloric Acid (to adjust pH), Purified Water.
Privine Nasal: Dibasic Sodium Phosphate, Disodium Edetate, Monobasic Sodium Phosphate, Purified Water, Sodium Chloride

>>Category:
Decongestant and Ophthalmic.

>>Mechanism of action:
- Naphazoline belongs to the imidazole group of sympathomimetics.
- It is a Vasoconstrictor of relatively long duration of action.
~> The drug directly stimulates �-adrenergic receptors in the arterioles of the conjunctiva and the nasal mucosa to produce vasoconstriction. It also exerts little or no effect on �-adrenergic receptors.
~> It shrinks the blood vessels found in the nose as well as elsewhere in the body.
> In the nose, this shrinkage:
     - Allows better drainage of the sinuses,
     - Improves the ease of breathing, and
     - Relieves the stuffy feeling.
> In the eye, topical application to the conjunctiva:
     - Shrinks the blood vessels,
     - Small arterioles are constricted, and
     - Conjunctival congestion is temporarily relieved.
*The drug also may produce mydriasis when applied to the conjunctiva, but this effect is usually minimal with the concentrations used as ocular decongestants.

>>Precautions to consider:

a. Allergic reactions:
- Chronic use of this medication may damage the blood vessels (veins and arteries) in the eyes. However, an overuse can increase the redness and irritation in the eye and can even lead to permanent damage.
- Naphazoline contains a preservative (Benzalkonium Chloride), which might discolor contact lenses, so wearing soft contact lenses when applying this medication should be avoided.
- An allergic reaction (dyspnea; closing of the throat; swelling of the lips, face, or tongue; or hives); might occur.

b. Pregnancy:
Naphazoline is in the FDA pregnancy category C (not known whether it can cause fetal harm when administered to a pregnant woman). Therefore, it should be used during pregnancy only when clearly needed.

c. Breast-feeding:
It is not known whether naphazoline passes into breast milk but because many drugs are distributed into milk, caution should be exercised when this drug is administered to a breast-feeding woman.

d. Drug interactions:

i. Drug-Drug interactions:
- Drug interactions between naphazoline ophthalmic and drugs taken by mouth are not expected but still they can occur.
It should be avoided with the following:
   1. Anesthetics (discontinue mydriatic prior to use of anesthetics that sensitize the myocardium to sympathomimetics, ie, cyclopropane, halothane).
   2. MAOI such as Isocarboxazid (Marplan), Tranylcypromine (Parnate), or Phenelzine (Nardil).
   3. Tricyclic antidepressants hypertensives (may potentiate the pressor effects of naphazoline).
   4. �-blocker such as propranolol (Inderal), metoprolol (Lopressor, Toprol XL), or labetalol (Normodyne, Trandate).

ii. Drug-Disease interactions:
- Use with caution in the presence of other medical problems:
> Hypertension.
> Diabetes Mellitus.
> Hyperthyroidism (the use of Naphazoline makes the condition worse).
> Heart Disease.
> Coronary Artery Disease.
> Cerebral Arteriosclerosis.
> Long-standing Bronchial Asthma.
> Eye disease, infection, or injury (the symptoms of the condition may be confused with possible side effects of ophthalmic Naphazoline).

e. Contra-indications:
- This drug is Contraindicated in:
1. Patients with known hypersensitivity to the drug.
2. Patients with glaucoma, they should be advised not to use the drug except under the advice and supervision of a physician.
3. Patients with angle-closure glaucoma; ophthalmic solutions of the drug should not be used.
4. Patients using soft contact lenses; fixed combinations containing naphazoline hydrochloride and antazoline are contraindicated while soft contact lenses are being worn.
5. Children (unless under medical supervision).

>>Side effects:

~> Overuse, long-term use or too frequent use may cause:
1. Increased eye irritation.
2. Irritation to the nasal mucosa or conjunctiva and, especially in children, adverse systemic effects.
3. Rebound congestion, characterized by chronic redness, swelling and rhinitis, following intranasal applications.
4. Reactive hyperemia following ophthalmic applications.
5. Increased or decreased intraocular pressure.
6. Mydriasis.
7. Blurred vision.
8. Systemic sympathomimetic effects such as:
   a. Hypertension and Headache.
   b. Cardiac irregularities.
   c. Nervousness and sweating.
   d. Nausea.
   e. Dizziness and weakness.

~> After intranasal application, it may cause:
1. Transient burning.
2. Stinging.
3. Dryness.
4. Ulceration of the mucosa.
5. Sneezing.
6. Occasionally anosmia.
7. Nausea.
8. Headache.
9. Drowsiness.

~> Overdosage of the drug may produce:
1. Drowsiness.
2. Decreased body temperature.
3. Bradycardia.
4. Shock-like hypotension and coma.

>>Patient consultation:

>For the eye:
- Eye drops need to be kept sterile.
- When putting them the eye,
- Wash the hands, tilt back the head, and pull the lower eyelid away from the eye forming a pocket.
- Drop the medication in the pocket and close the eyes for several minutes.
- Do not blink.

>For the nose:
- Blow the nose gently to clear it.
- Tip the head back.
- Instill the prescribed number of drops into each nostril.
- Keep the head tilted back for several minutes.
- Rinse the dropper in hot water and dry it with a clean tissue.

* Missed dose should be used as soon as remembered but,
1. Skip the missed dose and resume your usual dosing schedule.
2. Do not "double-up" the doses.

* If eye pain or change in vision occurs or if redness or irritation of the eye continues, gets worse, or lasts for more than 72 hours, stop using the medicine and check with your doctor.

* Dosing consideration:
1. Naphazoline ophthalmic can be used up to four times a day q3h or q4h
2. Do not use this drug continuously for longer than 48 to 72 hours without consulting your doctor.
* Overdosing and emergency:
1. If you do suspect an overdose, wash the eye with water and call an emergency room or poison control center near you.
2. If the drops have been ingested (taken by mouth), drink plenty of fluid and call an emergency center for advice.

* Remove contact lenses before administering this medication.
* Do not use the solution if it becomes cloudy or changes color.

>>Uses and general dosing information:

>Uses:
- Naphazoline is used as:
1. Topical ocular vasoconstrictor.
2. Nasal decongestant. Decongestion in both the eye and nose by constricting blood vessels.
3. Enlarges the pupil.
4. Reduction in the amount of fluid in the eye, either by:
         a. Reducing the production of fluid inside the eye.
OR    b. Increasing the amount of fluid that drains from the eye.

- Naphazoline relieves:
1. Redness.
2. Burning.
3. Irritation.
4. Dryness of the eye caused by wind, sun, and other minor irritants.

>Dosing information:

*Ophthalmic:
- Not recommended due to CNS depression (especially in infants).
- Instill 1-2 drops into conjunctival sac of affected eye(s) every 3-4 hours.
- Therapy generally should not exceed 3-4 days.
* Strength:
012% (7.5 mL, 30mL), 0.02% (15 mL), 0.03% (15 mL), 0.1% (15 mL).

*Nasal: <Intranasal>
- Not recommended due to CNS depression (especially in infants)
- Children:- 1 spray into each nostril every 6 hours if necessary.
                 - Therapy should not exceed 3-5 days.
- Children >12yrs and Adults: - Instill 1-2 drops or sprays every 6 hours if needed.
                                               - Therapy should not exceed 3-5 days
* Strength: Drops: 0.05% (20 mL).
                     Spray: 0.05%   (15 mL).

>>Sorage condition and labeling:
>To store this medicine:
    1. Keep out of the reach of children.
    2. Store at room temperature between 59 and 86 degrees F (15 to 30 degrees C) away from moisture and sunlight.
    3. Do not store in the bathroom.
    4. Keep the bottle properly capped.
    5. Keep the medicine from freezing.
    6. Do not keep outdated medicine or medicine no longer needed. Discard if drops become discolored or cloudy and be sure that any discarded medicine is out of the reach of children.

>>Any additional data:
- Excessive dosage of topical application of naphazoline hydrochloride may cause marked sedation in children.
- Nasal solutions containing 0.025 or 0.05% naphazoline hydrochloride shouldnot be used in children younger than 6 or 12 years of age, respectively, unless under the direction and supervision of a physician.
- One manufacturer states that 0.1% naphazoline hydrochloride ophthalmic solution is contraindicated in infants and children, since CNS depression possibly progressing to coma and hypothermia may occur in children, especially infants.

                    ______________________________________________________________________________

By: SH.Y.O

>>Reference:

. AHFS Drug Information 95, by Gerald K. Mcevoy. Pharm. D
. Martindale 30th edition, by james E.F Reynold's
. USP DI 1993, 13th edition
. Remington: The Science and practice of pharmacy, 1995 19th edition
. Internet: drugstore.com, healthsquare.com, medscape.com