Chemical formula: C₂₀H₃₃N₃O₄ Molecular mass: 379.501 g/mol PubChem compound: 2663
Celiprolol interacts in the following cases:
There is a theoretical risk that concurrent administration of monoamine oxidase inhibitors and high doses of beta-adrenoceptor blockers, even if they are cardio selective, can produce hypotension and is therefore not recommended.
Sympathomimetic agents, such as adrenaline, may counteract the effects of beta blockers.
The dosage of celiprolol should be reduced by half in patients with creatinine clearance values of 15-40 ml/minute, heart rate should be monitored and treatment should be reconsidered in case of bradycardia (less than 50-55 beats per minute at rest).
Beta blockers may intensify the blood sugar lowering effects of insulin and oral antidiabetic drugs, and the dosage of antidiabetics may therefore require adjustment. In addition, beta-adrenoceptor blockers may mask the symptoms of thyrotoxicosis or hypoglycaemia (in particular, tachycardia).
Digitalis glycosides, in association with beta-adrenoceptor blocking drugs, may increase A-V conduction time.
Care should be taken in prescribing beta-adrenoceptor blockers with Class I antiarrhythmic agents (e.g. disopyramide, quinidine) and amiodarone, since these agents may potentiate the negative effects on A-V conduction and myocardial contractility. Clinical and ECG monitoring must be performed.
Concomitant use of other antihypertensive agents, or of tricyclic antidepressants, barbiturates or phenothiazines, may potentiate the orthostatic hypotensive effects of beta blockers.
Concomitant therapy with dihydropyridine calcium channel antagonists, such as nifedipine, may increase the risk of hypotension, and cardiac failure may occur in patients with latent or uncontrolled cardiac insufficiency.
Blood pressure should be closely monitored in case of co-administration of celiprolol and dihydropyridine derivatives especially when therapy is initiated.
Beta blockers may exacerbate the rebound hypertension which can follow the withdrawal of clonidine. If the two drugs are co-administered, the beta-adrenoceptor blocking drug should be withdrawn several days before discontinuing clonidine.
In case of shock or hypotension due to floctafenine, beta-blockers may reduce the effectiveness of drugs used to compensate these symptoms.
Drugs inhibiting prostaglandin synthetase, such as ibuprofen or indometacin, may decrease the hypotensive effects of beta-adrenoceptor blocking drugs.
Concomitant therapy of celiprolol with mefloquine may cause bradycardia.
Calcium channel antagonists such as verapamil (and to a lesser extent diltiazem) and beta blockers both slow A-V conduction and depress myocardial contractility through different mechanisms. When changing from verapamil to celiprolol and vice versa, a period between stopping one and starting the other is recommended. Concomitant administration of both drugs is not recommended and should only be initiated with both clinical signs and ECG monitored carefully. Patients with pre-existing conduction abnormalities should not be given the two drugs together.
Due to its negative effect on conduction time, celiprolol should only be given with caution to patients with first degree heart block.
In patients with a history of anaphylactic reactions, beta blockers may increase the sensitivity to allergens and the seriousness of the reactions.
Celiprolol therapy must be reported to the anaesthetist prior to general anaesthesia. If it is decided to withdraw the drug before surgery, 48 hours should be allowed to elapse between the last dose and anaesthesia. Continuation of beta blockade reduces the risk of arrhythmias during induction and intubation, although reflex tachycardia may be attenuated and the risk of hypotension may be increased. In the event of continuation of celiprolol treatment special care should be exercised when using anaesthetic agents such as ether, cyclopropane or trichloroethylene. The patient may be protected against vagal reactions by the intravenous administration of atropine.
Caution should be observed in patients with diabetes mellitus as beta blockers may mask the symptoms of hypoglycaemia (in particular, tachycardia).
Beta blockers may increase the number and the duration of anginal attacks in patients with Prinzmetal’s angina, due to unopposed alpha-receptor mediated coronary artery vasoconstriction. The use of beta-1 selective adrenoceptor blocking drugs such as celiprolol may be considered in these patients, but the utmost care should be exercised.
Beta blockers have been reported to exacerbate psoriasis, and patients with a history of psoriasis should take celiprolol only after careful consideration.
Beta blockers may mask the symptoms of thyrotoxicosis.
The safety of this medicinal product for use in human pregnancy has not been established. An evaluation of experimental animal studies does not indicate direct or indirect harmful effects with respect to reproduction, development of the embryo or fetus, the course of gestation and peri- and post- natal development.
However, beta-adrenoceptor blocking drugs in general have been associated with reduced placental perfusion, which may result in intrauterine fetal death, immature and premature deliveries. Celiprolol should therefore not be used during pregnancy unless there is no safer alternative.
In the newborn of treated mothers, beta-blocking activity persists for several days after birth and this may result in an increased risk of cardiac and pulmonary complications in the neonate in the post-natal period.
In general beta blockers reduce placental perfusion, which may result in intrauterine foetal death, immature and premature deliveries. Plasma volume should not be increased as risk of acute pulmonary oedema may exist. In addition, adverse effects (especially hypoglycaemia, bradycardia and respiratory distress) may occur in foetus and neonate. Therefore close monitoring of the neonate is recommended for the first 3 to 5 days of life.
When given within 48 hours of delivery of an obstetric patient, hypotension and bradycardia may be seen in the infant.
Most beta blockers will pass into breast milk, although to variable extents. There is insufficient information on the excretion of celiprolol in human milk.
The risk of hypoglycaemia and bradycardia occurring in the nursing infant have not been evaluated. A risk to the newborns/infants cannot be excluded.
The use of celiprolol is therefore not recommended in breast-feeding mothers.
It has been shown that driving ability is unlikely to be impaired in patients taking celiprolol. However, it should be taken into account that occasional dizziness or fatigue may occur as well as the potential for tremor, headaches or impaired vision. If affected, patients should be advised not to drive or operate machines.
Beta-adrenoceptor blockers may mask the symptoms of thyrotoxicosis or hypoglycaemia (in particular, tachycardia).
Occasional side effects, which are usually mild and transient have occurred. These include headache, hot flushes, asthenia, dizziness, fatigue, somnolence and insomnia (sleep disturbances). Additional side effects associated with beta-2 agonist activity, tremor and palpitations, have been reported. These effects usually do not require withdrawal of therapy.
Bronchospasm, skin rashes and/or visual disturbances have been reported in association with the use of beta blockers. Celiprolol should be discontinued if these effects occur.
The following undesirable effects have been observed during treatment with celiprolol and other beta-blockers with the following frequencies.
The frequencies of adverse events are ranked according to the following: Very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10,000, <1/1000), very rare (<1/10,000), Not known (cannot be estimated from available data).
Not known: Hypoglycaemia, Hyperglycaemia
Latent diabetes mellitus may come to light, and apparent diabetes mellitus may worsen.
Beta-blockers may mask the symptoms of hypoglycaemia or thyrotoxicosis (in particular tachycardia and tremor).
Common: depression has been reported.
Uncommon: insomnia
Very rare: psychoses
Not known: hallucinations, nightmare, libido decrease
Common: headache and dizziness, somnolence, nightmares and insomnia (sleep disturbances), tremor and sensation of coldness in the extremities have been reported, paraesthesia, asthenia.
Very rare: confusion
Not known: syncope
Not known: impaired vision, visual disturbances have been reported including xerophthalamias; dry eyes (to be considered if the patient uses contact lenses).
Rare: tinnitus
Common: significant decrease in blood pressure including when standing up from a lying position (orthostatic hypotension), have been reported.
Uncommon: palpitations
Rare: slowed AV-conduction, increased cardiac insufficiency with peripheral oedema and/or exertional dyspnoea. Heart failure, cold and cyanotic extremities. In susceptible patients: precipitation of existing A-V block.
Not known: bradycardia, cardiac failure
Common: Hot flush, In susceptible patients: exacerbation of intermittent claudication Raynaud’s disease or syndrome have been reported.
Uncommon: Cold extremities, hypotension
Uncommon: Dyspnoea
Rare: hypersensitivity pneumonitis, asthmatic dyspnoea especially in patients with bronchial asthma or a history of asthmatic complaints.
Not known: Interstitial pneumonitis, bronchospasm
Common: nausea, vomiting, abdominal pain and abdominal discomfort can occur, dry mouth
Rare: constipation.
Not known: diarrhoea.
Not known: Increase in transaminases
Common: rash, pruritus, hyperhidrosis, erythema
Rare: allergic skin reactions (e.g. itching, flush, rash, pruritus, urticaria, purpura).
Very rare: Beta blockers can cause psoriasis in isolated cases, worsen the symptoms of this disease or lead to the formation of psoriasiform exanthemes.
Common: muscle cramps
Uncommon: arthralgia
Rare: muscle weakness
Not known: systemic lupus erythmatosus
Common: erectile dysfunction
Rare: male impotence, libido decrease
Common: fatigue.
Common: An increase in antinuclear antibodies (ANA) has been seen, its clinical relevance is not clear.
Antinuclear antibodies have been observed, exceptional and reversible lupus syndrome
Not known: hepatic transaminases increased
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