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Thursday 8 December 2011

what is Atenolol?

Atenolol is used as a racemate. The formulas show the (R)-enantiomer and above the (S)-enantiomer below.

Drug class

β-Adrenozeptorenblocker (beta blockers)
Finished products (selection)

Atebeta ®
Atenogamma ®
Atenolol STADA ®
Effect

Atenolol is a hydrophilic beta-receptor blocker with relative selectivity for β1 (cardioselectivity), without intrinsic sympathomimetic activity (ISA) and without membrane-stabilizing effect. The substance has hypotensive and antiarrhythmic.

Mechanism of action

General information about the mechanism of action of beta blockers can be found here.

Atenolol is a hydrophilic beta-receptor blocker with relative selectivity for β1 (cardioselectivity) without intrinsic sympathomimetic activity (ISA). Atenolol different from other beta-blockers by its low lipophilicity, therefore, the substance has a low permeability to the central nervous system and therefore shows no membrane-stabilizing effect.
The β1-selectivity decreases with increasing dose. The dose-response curve is flat in the therapeutic range.
The substance lowers depending on the level of sympathetic tone, the frequency (negative chronotropic) and force of heart contraction (negative inotropic effect), the AV conduction velocity, and plasma renin activity. Atenolol can cause inhibition of β2-receptors by increasing the tone of smooth muscles.
Occurs when an increase of airway resistance, atenolol should be discontinued and a bronchodilatative therapy (eg salbutamol) was initiated.
Atenolol reduces heart rate and blood pressure. It increases the AV conduction time, the refractory period of the atrium and the atrioventricular node. The blood pressure reduction by atenolol is quickly absorbed and reaches the full extent after a week. Concomitant administration of other antihypertensives reinforces the therapeutic effect. Pulse rate and blood pressure spikes during treatment with atenolol largely avoided. The early use of atenolol in acute myocardial infarction reduces infarct size and decreases the morbidity and mortality. Patients at risk of heart attack less likely to develop definite infarction, the incidence of ventricular arrhythmias is less pronounced and the pain relief leads to a reduction in analgesic requirements.
Atenolol is in most ethnic groups, effective and well tolerated, although black patients may respond less strongly. It is unlikely that additional properties of (S )-(-) atenolol, compared with the racemate lead to different therapeutic effects would be.
Because of their negative inotropic effect, the use of beta blockers in non-compensated heart failure can be avoided.

Contraindications (contraindications)

The following are absolute Gegenanzeiegn (situations in which the drug should be administered in any case) and relative contraindications (situations in which the drug should be administered with caution) listed. For more information or answers to your questions please use the forum or ask your doctor or pharmacist.

Absolute contraindications
- Overt cardiac failure;
- Shock;
- AV-block II or III. Degree;
- Sino-atrial block;
- Sinus node disease (sick sinus syndrome);
- Bradycardia (resting heart rate <50 beats / min prior to treatment);
- Hypotension (systolic less than 90 mm Hg);
- Late stages of peripheral vascular disease;
- Bronchial hyper-reactivity (eg asthma);
- Acidosis;
- Hypersensitivity to atenolol or other beta-receptor blockers

Relative contraindications
- Psoriasis in a personal or family history;
- First degree AV block (due to the negative effect on the electrical conduction);
- Diabetic patients with widely fluctuating blood sugar levels, state after prolonged fasting, severe, or severe physical stress (risk of severe hypoglycemic states), the hypoglycemic tachycardia can be modified.
- Pheochromocytoma (adrenal gland tumor), prior therapy with α-receptor blockers is required;
- Impaired renal function;
- Prinzmetal's angina (risk of gain) due to unhindered α-receptor-mediated vasoconstriction of the coronary arteries can increase the number and duration of seizures in patients;
- A history of severe hypersensitivity reactions, simultaneous desensitization (risk of increased sensitivity to allergens and the severity of anaphylactic reactions);
- Ease of peripheral vascular disease;
- Pregnancy;
- Breast-feeding

Side effects (adverse reactions)

This is a complete list of the known side effects, for more information or answers to your questions please use the forum or ask your doctor or pharmacist.

 
 

Adverse effects, without specifying the frequency
- Concealment of the warning signs of hypoglycemia (tachycardia, tremor);
- Hypoglycemic state after prolonged fasting or strict association with heavy physical load;
- Disturbances in lipid metabolism (decrease in HDL-cholesterol, increased triglycerides in plasma, mostly normal total cholesterol);
- Concomitant hyperthyroidism: obscuring the signs of thyrotoxicosis (eg, tachycardia, tremor);
- Severe liver damage.

Common adverse reactions (> 1 / 100)
- Bradycardia;
- Cold feeling in the extremities;
- Dizziness;
- Sweating;
- Fatigue;
- Gastrointestinal complaints (nausea, vomiting, constipation, diarrhea).

Uncommon adverse reactions (> 1 / 1000)
- Increased dream activity;
- Insomnia;
- Increased transaminase;
- Conjunctivitis;
- Muscle weakness;
- Muscle cramps;
- Manifestation of a latent or manifest diabetes mellitus, exacerbation of.

Rare adverse reactions (> 1 / 10000)
- Strengthening of heart failure;
- Atrioventricular conduction disturbances;
- With orthostatic hypotension or syncope;
- Strengthening of pre-existing symptoms in peripheral vascular disease (intermittent claudication, Raynaud's syndrome);
- Dizziness;
- Confusion;
- Hallucinations;
- Psychosis;
- Paresthesia,
- Headache;
- Depression;
- Nightmares;
- Dry mouth;
- Liver damage including intrahepatic cholestasis.
- Purpura;
- Thrombocytopenia;
- Allergic reactions such as erythema, pruritus, rash;
- Loss of hair;
- Triggering or worsening of psoriasis or psoriasiform eruptions triggering;
- Libido, impotence;
- Shortness of breath, especially with pre-existing tendency to bronchospastic reactions, especially for obstructive airway diseases;
- Blurred vision;
- Decreased lacrimation (contact lenses).

Very rare adverse reactions (<1 / 10000)
- Strengthening of existing seizures in angina pectoris;
- Strengthening of allergic reactions that do not respond to the usual adrenaline doses;
- Increase in ANA titer, clinical significance remains unclear;
- Worsening of preexisting renal dysfunction.

Sunday 20 November 2011

beta blockers and atenolol

Information on beta blockers and atenolol. Medication to treat blood pressure.