Drug reference

Celiprolol

Beta-1 selective adrenergic blocker with partial β2-agonist activity · Antihypertensive

Also known as Celiprolol hydrochloride

START

200 mg PO once daily; 200 mg twice daily for vEDS

TYPICAL MAX

400 mg/day

STOP IF

Severe bradycardia / heart block or asthma exacerbation

WATCH

HR, BP, asthmatic symptoms, electrolyte / glycaemia in diabetics

CDSCO approvedSchedule HATC C07AB08

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 1h · absorption
PEAK: 3h · Tmax
t½: 5h · t½
DURATION: 1d · once-daily

EXCRETION

Renal — mainly unchanged

route + CYP

INTERACTIONS

10 major

incl. contraindicated

PREGNANCY

Use only if clearly needed; β-blocker class — IUGR risk.

FDA category + note

Top interactionssee all 12 →

DiltiazemContraindicatedTextbookG&G 14e · p617
RitodrineContraindicatedTextbookKDT 7e · p333
AdrenalineSevereTextbookKDT 7e · p133
AmilorideSevereTextbookKDT 7e

Mechanism

Cardio-selective β1-receptor antagonist with intrinsic sympathomimetic activity at β2 receptors → mild peripheral vasodilation; no negative effects on lipid profile and possibly favourable in vascular Ehlers-Danlos syndrome (vEDS).

Indications

HypertensionStable angina pectorisVascular Ehlers-Danlos syndrome (off-label / European; reduces arterial events)

Dosing

Adult: Hypertension/angina: 200 mg PO once daily; up to 400 mg once daily. vEDS: 200 mg PO twice daily.
Pediatric: Not established.
Renal adjustment: CrCl 15–40: reduce by 50%; CrCl <15: avoid.
Hepatic adjustment: Caution; reduce in significant hepatic impairment.
Geriatric: Start 100 mg/day; titrate slowly.
Max dose: 400 mg/day (HTN/angina); 400 mg/day (vEDS in divided doses)

Pharmacokinetics

Onset

BP / HR effect over hours

Peak effect

~3 h (Tmax)

Duration

~24 h

Half-life

~5 h

Bioavailability

~30–70%

Protein binding

~25%

Metabolism

Minimal hepatic

Excretion

Renal (mainly unchanged)

Contraindications

Cardiogenic shock
Severe heart failure (untreated)
Second/third-degree AV block (no pacemaker)
Bradycardia / sick sinus syndrome
Severe asthma
Hypersensitivity

Side effects

Common

FatigueDizzinessHeadacheSleep disturbanceBradycardia

Serious

Severe bradycardia / heart block
Bronchospasm (less than non-selective)
Heart failure exacerbation
Masked hypoglycaemia signs in diabetics

Pregnancy & lactation

Pregnancy

Use only if clearly needed; β-blocker class — IUGR risk.

Lactation

Excreted in milk; monitor infant for bradycardia/hypoglycaemia.

Drug interactions

Diltiazem

Contraindicated

Textbook

Increased propensity for AV block, severe bradycardia, and decreased left ventricular function.

Avoid concurrent administration. The concurrent administration of diltiazem with a beta blocker is contraindicated.

Source: G&G 14e · p617

Ritodrine

Contraindicated

Textbook

Reduced efficacy of ritodrine and potential for adverse cardiovascular effects.

Ritodrine should not be used if the mother is receiving beta blockers.

Source: KDT 7e · p333

Adrenaline

Severe

Textbook

Marked rise in BP.

Adrenaline should not be given to patients receiving β blockers.

Source: KDT 7e · p133

Amiloride

Severe

Textbook

Hyperkalaemia more likely.

Source: KDT 7e

Epinephrine

Severe

Textbook

Severe hypertension and cerebral hemorrhage.

The use of epinephrine generally is contraindicated in patients who are receiving nonselective β receptor antagonists.

Source: G&G 14e · p258

Methacholine

Severe

Textbook

Exaggerated or prolonged bronchoconstriction and reduction in vital capacity in response to methacholine.

Emergency resuscitation equipment, oxygen, and medications to treat severe bronchospasm (e.g., β2 adrenergic receptor agonists for inhalation) should be available during testing.

Source: G&G 14e · p212

Sofosbuvir

Severe

Textbook

Severe bradycardia.

Extreme caution advised if amiodarone is co-administered with sofosbuvir and a beta blocker.

Source: Harrison 22e · unknown

Triamterene

Severe

Textbook

Hyperkalaemia more likely.

Source: KDT 7e