1. Alkindey Teaching Hospital
Department of clinical pharmacy
Clinical pharmacy training program
Post graduated year 1
Obstetric and gynecology ward
Group (2)
Antihistamines and decongestants
safety in breast feeding
2. Antihistamines and breast feeding
Milk levels of first generation antihistamines are low or unknown. Nonetheless,
effects such as irritability, excessive crying and sleep disturbances in the infant
have been reported and there is a small chance these agents may reduce milk
supply. Occasional small doses are not expected to be harmful.
Second generation antihistamines also are not expected to be harmful during
lactation and tend to be preferred because of lack of sedative effects.
Recommendation:
The first generation antihistamines, especially chlorpheniramine, are preferred in
pregnancy; if these are not tolerated or effective, second generation agents such
as loratadine can be recommended. Due to possible effects on the infant from
first generation antihistamines, second generation agents are preferred in
lactating mothers.
3. Phenyltoloxamine is an antihistamine with
analgesic properties used in over-the counter
preparations. There are no reports describing the use
of phenyltoloxamine during human lactation or
measuring the amount.
Pyrilamine is an antihistamine which blocks the H1
receptor. It is used in many over-the-counter products.
Antihistamines in this class may cause excitement or
sleeplessness in children. Use of these older
antihistamines in pregnant and breastfeeding mothers
should be avoided.
Triprolidine is an antihistamine. It is secreted into
milk but in very small levels and is marketed with
pseudoephedrine as Actifed. The relative infant dose is
less than 1.8% of the weight-normalized maternal
dose. This dose is far too low to be clinically relevant.
4. Azelastine (Astelin) is an antihistamine for oral,
intranasal and ophthalmic administration. It is effective
in treating seasonal and perennial rhinitis and nonallergic
vasomotor rhinitis. Ophthalmically, it is effective for
allergic conjunctivitis (itchy eyes). However, this is an
extremely bitter product. It is possible that even
minuscule amounts in milk could alter the taste of milk
leading to rejection by the infant.
Brompheniramine is a popular antihistamine
typically sold in combination cough and cold products.
Although only insignificant amounts of brompheniramine
appear to be secreted into breast milk, there are a
number of reported cases of irritability, excessive crying
and sleep disturbances that have been reported in
breastfeeding infants.
5. Carbinoxamine is an antihistamine used over-the-
counter. The main adverse effect is sedation. The use
of this sedating antihistamine in breastfeeding mothers
is not ideal. Non-sedating antihistamines are generally
preferred.
Cetirizine is a popular new antihistamine useful for
seasonal allergic rhinitis. It is a metabolite of
hydroxyzine and is one of the most potent of the
antihistamines. It penetrates the CNS poorly and
therefore produces minimal sedation.
6. Chlorpheniramine is a commonly used
antihistamine. Although no data are available on
secretion into breast milk, it has not been reported to
produce side effects.
Cyproheptadine is a serotonin and histamine
antagonist with anticholinergic and sedative effects. It
has been used as an appetite stimulant in children
and for rashes and pruritus (itching). No data are
available on its transfer to human milk. The main
adverse effect to watch out for is sedation.
7. Desloratadine is the active metabolite of loratadine and its half-
life is longer than the parent compound. While we do not have
specific data on desloratadine, we do have a good report on the
prodrug loratadine.
Dexbrompheniramine is a first-generation antihistamine with
anticholinergic properties. Due to the fact that
dexbrompheniramine is well-absorbed and has a long half-life, it is
likely secreted into human milk
Diphenhydramine is an antihistamine used for allergic
conditions. It is also used as a sleep aid and as an antiemetic
agent for the prevention of motion sickness. This sedating
antihistamine should only be used for a short duration in
breastfeeding mothers. Non-sedating antihistamines are
generally preferred. There are reports that diphenhydramine
suppresses milk production.
8. Fexofenadine is a non-sedating histamine-1 receptor
antagonist and is the active metabolite of terfenadine. It is
indicated for symptoms of allergic rhinitis and other
allergies. Unlike terfenadine, no cardiotoxicity has been
reported with this product. The authors estimate that only
0.45% of the weight-adjusted maternal dose would be
ingested by the infant.
Ketotifen is a second-generation H1 antihistamine. It is
used ophthalmically to treat red eye and allergic
conjunctivitis. Ketotifen has been shown to enter breast milk
in animal studies; however, it is unknown if it is excreted into
human breast milk. It is unknown if enough drug enters
systemic circulation after topical administration to produce
significant quantities in breast milk.
9. Levocetirizine is a third-generation non-sedating
antihistamine. No data on the transfer into human milk are
available at this time. Just as with cetirizine, it is probably
compatible with breastfeeding.
Loratadine is a long-acting antihistamine with minimal
sedative properties. According to the authors, a 4 kg infant
would receive only 2.9 μg/kg of loratadine. It is very unlikely
this dose would present a hazard to breastfed infants. The half-
life in neonates is not known although it is likely quite long.
Pediatric formulations are available.
10. Pheniramine is an antihistamine used for allergic rhinitis and
conjunctivitis. There are no adequate and well-controlled
studies or case reports in breastfeeding women. Since this is an
antihistamine, it may cause sedation in the breastfed infant.
Caution is advised, especially in premature infants and
newborns. Consider non-sedating anti-histamines such as
cetrizine or loratidine as alternatives.
Meclizine is an antihistamine frequently used for nausea,
vertigo and motion sickness although it is inferior to
scopolamine. Meclizine was previously used for nausea and
vomiting of pregnancy in the U.S., and still is in many countries.
No data are available on its secretion into breast milk. The use
of meclizine while breastfeeding is probably safe; however
monitoring for sedation in the infant is advised.
11. Sedating antihistamines if taken for more than 3 days may
cause lowered milk supply due to drowsiness and less
frequent feeding by the baby
Non sedating antihistamines can be taken by breastfeeding
women outside of license application. Most are licensed for
paediatric doses e.g. loratadine and cetirizine
Eye drops and nasal sprays reach low levels in breast milk
and can be used as normal
12. Decongestants and breast feeding
Adverse effects of systemic decongestants on the nursing infant are unlikely,though
irritability has been reported occasionally in association with pseudoephedrine.
Concern regarding systemic decongestants is the potential to reduce milk supply in
the breastfeeding mother. Single 60mg doses of pseudoephedrine have reduced
supply by over 20% within 24 hours of its use; phenylephrine is thought to act
similarly, though no data exists.Therefore, these drugs need to be used with caution
in mothers with poor or marginal milk supply,including those whose milk supply has
not been established (which may take up to six to eight weeks postpartum)and those
in late-stage lactation.
No data exist concerning the use of topical decongestants in lactation. However,
experts suggest oxymetazoline is unlikely to be harmful to the infant, and it is
suggested by some as first line pharmacotherapy.
13. Xylometazoline is a vasoconstrictive agent used both nasally
and ophthalmically. No reports are available regarding the use of
xylometazoline during lactation and effects on the infant with
exposure of the drug in human milk are unknown.
Xylometazoline may be absorbed systemically when used nasally.
Caution is warranted when contemplating use of xylometazoline
while breastfeeding.
Pseudoephedrine is an adrenergic compound primarily used as
a nasal decongestant. It is secreted into breast milk but in low
levels. The calculated dose that would be absorbed by the infant
is very low (0.4 to 0.6% of the maternal dose). Therefore,
breastfeeding mothers with poor or marginal milk production
should be cautious in using pseudoephedrine. While there are
anecdotal reports of its use in mothers with engorgement, we do
not know if it is effective, or recommend its use for this purpose
at this time.
14. Levmetamfetamine is used as a nasal decongestant for
the temporary relief of nasal congestion due to a cold, hay
fever, or other upper respiratory allergies. While it produces
local vasoconstriction, it has little CNS effects in humans.
There are no data on the use of this product in breastfeeding
women. Some will probably transfer into human milk,
although its oral absorption is probably low and the clinical
side effects in an infant are probably minimal.
Naphazoline is used for relief of red eyes and as a nasal
decongestant (spray). Over the counter products have low
naphazoline concentrations (0.05%) such that systemic
absorption is probably low, especially from ophthalmic
preparations. There are no adequate or well-controlled
studies in breastfeeding women; however, the risk of side
effects to a breastfed infant is probably minimal
15. Oxymetazoline is a decongestant. No adequate
well-controlled studies exist on the use of
oxymetazoline during breastfeeding; however, very
little oxymetazoline is expected to reach the infant
through breast milk due to its local administration and
limited absorption. Oxymetazoline has been preferred
over oral systemic decongestants such as
pseudoephedrine during breastfeeding. Oxymetazoline
should only be used briefly, no more than 3 days
16. Phenylephrine is a sympathomimetic agent most commonly
used as a nasal decongestant due to its vasoconstrictive
properties but also for treatment of ocular uveitis,
inflammation and for cardiogenic shock. Phenylephrine is most
commonly added to cold mixtures and nasal sprays for use in
respiratory colds, flu and congestion. Used ophthalmically in
eye exams, the maternal dose of the medication would be very
low and it is not likely to pose a problem for a breastfeeding
infant. Although no data are available on its secretion into
human milk, probably very small amounts will be transferred
into milk. Due to phenylephrine’s poor oral bioavailability
(38%), it is not likely to produce clinical effects in a breastfed
infant unless the maternal doses were quite high.
