Hydralazine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Hypertensive crisis
Adult: Initially, 5-10 mg via slow inj, may repeat after 20-30 minutes if necessary. Alternatively, via infusion at a rate of 0.2-0.3 mg/min. Maintenance: 0.5-0.15 mg/min.

Oral
Congestive heart failure
Adult: In combination with nitrate: Initially, 25 mg 3-4 times daily, may increase dose every 2 days if necessary. Maintenance: 50-75 mg 4 times daily.

Oral
Hypertension
Adult: In combination with ß-blockers and diuretics: Initially, 25 mg bid, increase gradually according to response. Max: 200 mg daily.
Renal Impairment
CrCl (mL/min) Dosage
<30
Adjust dose or dosing interval according to clinical response.
Hepatic Impairment
Adjust dose or dosing interval according to clinical response.
Cách dùng
Should be taken with food.
Hướng dẫn pha thuốc
IV inj: Reconstitute vial labelled as containing 20 mg with 1 mL sterile water for injection; further dilute with 10 mL NaCl 0.9%. IV infusion: Add reconstituted IV inj to 500 mL NaCl 0.9%, sorbitol 5% solution or Ringers solution.
Chống chỉ định
Idiopathic systemic lupus erythematosus (SLE) and related diseases, severe tachycardia, heart failure associated with high cardiac output(e.g. thyrotoxicosis), myocardial insufficiency due to mechanical obstruction (e.g. aortic or mitral stenosis or constrictive pericarditis), cor pulmonale, dissecting aortic aneurysm, coronary artery disease (CAD), mitral valvular rheumatic heart disease, porphyria.
Thận trọng
Patient with cerebrovascular disease, suspected CAD, mitral valvular disease. Slow acetylators. Renal and hepatic impairment. Pregnancy and lactation. Avoid abrupt withdrawal.
Phản ứng phụ
Significant: SLE-like syndrome, blood dyscrasias (e.g. reduction in Hb and RBC count, leucopenia, agranulocytosis, purpura), postural hypotension, peripheral neuritis, anginal attacks, ECG changes.
Cardiac disorders: Tachycardia, palpitation.
Gastrointestinal disorders: Diarrhoea, nausea, vomiting, paralytic ileus, constipation.
Metabolism and nutrition disorders: Anorexia, oedema.
Musculoskeletal and connective tissue disorders: Arthralgia, joint swelling, myalgia.
Nervous system disorders: Headache, dizziness.
Renal and urinary disorders: Reduced urinary volume.
Vascular disorders: Flushing, orthostatic hypotension.
IM/IV/Parenteral/PO: C
Thông tin tư vấn bệnh nhân
This drug may cause dizziness or hypotension, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor blood pressure and heart rate; CBC and antinuclear antibody (ANA) titer prior to therapy and periodically thereafter; urine analysis at intervals of approx 6 months during long-term treatment.
Quá liều
Symptoms: Pronounced hypotension and tachycardia, headache, flushing, myocardial ischaemia, cardiac arrhythmias, shock, coma. Management: Symptomatic and supportive treatment. Perform gastric lavage or give emetic treatment in conscious patients as soon as possible. Administer IV fluids or plasma expander as needed. May administer angiotensin or norepinephrine IV to raise blood pressure with caution, avoiding precipitation or aggravation of cardiac arrhythmia or tachycardia.
Tương tác
Enhanced hypotensive effect with other antihypertensive agents (e.g. vasodilators, Ca channel blockers, ACE inhibitors, diuretics), anaesthetics, TCA (e.g. imipramine, clomipramine), major tranquilisers, nitrates or CNS depressants. May cause marked hypotension with diazoxide. May increase bioavailability of β-blockers (e.g. propranolol). Antagonised hypotensive effect with oestrogens and NSAIDs (e.g. ibuprofen, diclofenac).
Food Interaction
Enhanced hypotensive effect with alcohol.
Tác dụng
Description: Hydralazine is a direct-acting vasodilator which acts predominantly on the arterioles. The exact mechanism of action is unknown, but it is thought to exert its vasodilating effect through direct relaxation of vascular smooth muscle by inhibition of Ca release from the sarcoplasmic reticulum and inhibition of myosin phosphorylation in the arterial smooth muscle cells.
Onset: 10-80 minutes (IV).
Duration: Up to 12 hours (IV/IM).
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Bioavailability: Approx 22-69%, depending on acetylator status. Time to peak plasma concentration: 1-2 hours (oral).
Distribution: Crosses placenta, enters breastmilk (small amounts). Plasma protein binding: 87%.
Metabolism: Undergoes extensive first-pass metabolism in the liver via acetylation.
Excretion: Via urine as metabolites. Elimination half-life: 3-7 hours.
Đặc tính

Chemical Structure Image
Hydralazine

Source: National Center for Biotechnology Information. PubChem Database. Hydralazine, CID=3637, https://pubchem.ncbi.nlm.nih.gov/compound/Hydralazine (accessed on Jan. 23, 2020)

Bảo quản
Tab: Store between 15-30°C. IV inj: Store between 20-25°C. Protect from light.
Phân loại MIMS
Phân loại ATC
C02DB02 - hydralazine ; Belongs to the class of hydrazinophthalazine derivatives. Used in the treatment of hypertension.
References
Anon. Hydralazine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/11/2019.

Buckingham R (ed). Hydralazine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/11/2019.

Hydralazine Injection (Fresenius Kabi USA, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/11/2019.

Hydralazine Tablet (Camber Pharmaceuticals, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/11/2019.

Joint Formulary Committee. Hydralazine Hydrochloride. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/11/2019.

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