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Midodrine (brand names Amatine, ProAmatine, Gutron) is a vasopressor/antihypotensive agent. Midodrine was approved in the United States by the Food and Drug Administration (FDA) in 1996 for the treatment of dysautonomia and orthostatic hypotension. In August 2010, the FDA proposed withdrawing this approval because the manufacturer, Shire plc, has failed to complete required studies after the medicine reached the market.^[1]^[2]

In September 2010, the FDA reversed its decision to remove Midodrine from the market and has allowed it to remain available to patients while Shire plc collects further data regarding the efficacy and safety of the drug.^[3] Shire plc announced on September 27, 2011 that it was continuing the process to work with the FDA towards a final approval of the drug.^[4]

Chemical properties[edit]

Midodrine is an odorless, white, crystalline powder, soluble in water and sparingly soluble in methanol.

Mechanism of action[edit]

Midodrine is a prodrug which forms an active metabolite, desglymidodrine, which is an α₁-receptor agonist and exerts its actions via activation of the alpha-adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation of blood pressure. Desglymidodrine does not stimulate cardiac beta-adrenergic receptors. Desglymidodrine diffuses poorly across the blood–brain barrier, and is therefore not associated with effects on the central nervous system.

Metabolite desglymidodrine

Metabolism[edit]

After oral administration, midodrine is rapidly absorbed. The plasma levels of the prodrug peak after about half an hour, and decline with a half-life of approximately 25 minutes, while the metabolite reaches peak blood concentrations about 1 to 2 hours after a dose of midodrine and has a half-life of about 3 to 4 hours. The absolute bioavailability of midodrine (measured as desglymidodrine) is 93%.

Indications[edit]

Midodrine hydrochloride tablets are indicated for the treatment of symptomatic orthostatic hypotension. In a critical care setting, it is widely used as an adjunctive therapy to weaning patients off of intravenous vasopressive medications. It has been suggested also as a treatment for chronic fatigue syndrome^[5] as well as for hepato-pulmonary syndrome. It is also used with octreotide for hepatorenal syndrome; the proposed mechanism is constriction of splanchnic vessels and dilation of renal vasculature.

Contraindications[edit]

Midodrine is contraindicated in patients with severe organic heart disease, acute renal disease, urinary retention, pheochromocytoma or thyrotoxicosis. Midodrine should not be used in patients with persistent and excessive supine hypertension.

Side effects[edit]

Headache; feeling of pressure/fullness in the head, vasodilation/flushing face, confusion/thinking abnormality, dry mouth; nervousness/anxiety and rash.^{[citation needed]}

References[edit]

^ U.S. proposes withdrawal of Shire hypotension drug, Aug 16, 2010.
^ O'Riordan, Michael. "FDA recommends withdrawal of midodrine". Food and Drug Administration. FDA proposes withdrawal of low blood pressure drug [press release]. August 16, 2010. TheHeart.org. Retrieved 1 April 2011. .
^ Midodrine (ProAmatine, generic) Proposed Market Withdrawal – Update September 10, 2010.
^ Shire Announces Update on ProAmatime September 27, 2011.
^ Naschitz J, Dreyfuss D, Yeshurun D, Rosner I (April 2004). "Midodrine treatment for chronic fatigue syndrome". Postgrad Med J 80 (942): 230–2. doi:10.1136/pgmj.2003.011429. PMC 1742969. PMID 15082846.

External links[edit]

Midodrine at drugs.com

UpToDate Contents

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1. 起立性低血圧および食後低血圧の治療 treatment of orthostatic and postprandial hypotension
2. 血液透析時の血行動態の不安定性：概要 hemodynamic instability during hemodialysis overview
3. シェーグレン症候群による全身および腺外症状の治療 treatment of systemic and extraglandular manifestations of sjogrens syndrome
4. 肝腎症候群 hepatorenal syndrome
5. 肝硬変患者における腹水の治療：利尿剤抵抗性腹水 ascites in adults with cirrhosis diuretic resistant ascites

English Journal

Therapeutic response to vasoconstrictors in hepatorenal syndrome parallels increase in mean arterial pressure: a pooled analysis of clinical trials.

Velez JC, Nietert PJ.SourceDivision of Nephrology, Department of Medicine, Medical University of South Carolina, Charleston, SC.
American journal of kidney diseases : the official journal of the National Kidney Foundation.Am J Kidney Dis.2011 Dec;58(6):928-38. Epub 2011 Sep 29.
BACKGROUND: Vasoconstrictor therapy has been advocated as treatment for hepatorenal syndrome (HRS). Our aim was to explore across all tested vasoconstrictors whether achievement of a substantial increase in arterial blood pressure is associated with recovery of kidney function in HRS.STUDY DESIGN: P
PMID 21962618

Japanese Journal

Midodrine Hydrochloride Is Effective in the Treatment of Children With Postural Orthostatic Tachycardia Syndrome

CHEN Li,WANG Li,SUN Jinghui,QIN Jiong,TANG Chaoshu,JIN Hongfang,DU Junbao
Circulation journal : official journal of the Japanese Circulation Society 75(4), 927-931, 2011-03-25
… Background: The study was carried out to examine the effect of selective α1 adrenoceptor agonist midodrine hydrochloride vs. β-adrenergic blockade metoprolol in the treatment of children with postural orthostatic tachycardia syndrome (POTS). … Methods and Results: Fifty-three children with POTS were divided into group I (midodrine hydrochloride plus conventional therapy), group II (metoprolol plus conventional therapy) and group III (conventional therapy). …
NAID 10028103473

Related Pictures

Pillbox - National Library of Medicine Midodrine Hydrochloride Oral Tablet 5Mg Drug Medication Dosage Information US 5 212 Pill - midodrine 5 mg Midodrine Oral : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD

★リンクテーブル★

リンク元	「ミドドリン」
拡張検索	「midodrine hydrochloride」

「ミドドリン」

Midodrine
Systematic (IUPAC) name
	(RS)- N-[2-(2,5-dimethoxyphenyl)-2-hydroxyethyl]glycinamide
Clinical data
Trade names	Proamatine
AHFS/Drugs.com	monograph
MedlinePlus	a602023
Pregnancy cat.	?
Legal status	?
Identifiers
CAS number	133163-28-7
ATC code	C01CA17
PubChem	CID 4195
DrugBank	DB00211
ChemSpider	4050
UNII	6YE7PBM15H
KEGG	D08220
ChEBI	CHEBI:6933
ChEMBL	CHEMBL1076
Synonyms	2-amino-N-[2-(2,5-dimethoxyphenyl)-2-hydroxy-ethyl]-acetamide
Chemical data
Formula	C12H18N2O4
Mol. mass	254.282 g/mol
	SMILES O=C(NCC(O)c1cc(OC)ccc1OC)CN;
	InChI InChI=1S/C12H18N2O4/c1-17-8-3-4-11(18-2)9(5-8)10(15)7-14-12(16)6-13/h3-5,10,15H,6-7,13H2,1-2H3,(H,14,16) ; Key:PTKSEFOSCHHMPD-UHFFFAOYSA-N ;
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　　[★]

英: midodrine
化: 塩酸ミドドリン, midodrine hydrochloride
商: アバルナート、シュプレース、ナチルジン、ミドドリン塩酸塩、メトドリン、メトリジン、メトリジンD
関: アドレナリン受容体。血管収縮剤。

選択的α1アゴニスト。起立性低血圧の治療に用いられる。
ジメトキシフェニルアミノエタノール(DMAE)をグリシンで修飾したプロドラッグ。
肝、腎、空腸、血球など種々の臓器で脱グリシン化されて活性本体となり、交感神経α1-受容体を直接刺激し細動脈を収縮して全末梢血管抵抗を増大することにより血圧を上昇させる。
心機能にはほとんど影響せず、起立時の血圧低下を抑制する。
中枢への影響はなく、また正常血圧に影響を及ぼさない。
本態性低血圧症、起立性低血圧症の治療に用いられ、1日量4～8mgである。1回2-4mg 1日2回で用いられる。
禁忌：甲状腺機能亢進症、褐色細胞腫

「midodrine hydrochloride」

　　[★] ミドドリン、塩酸ミドドリン

[1] U.S. proposes withdrawal of Shire hypotension drug, Aug 16, 2010.

[2] O'Riordan, Michael. "FDA recommends withdrawal of midodrine". Food and Drug Administration. FDA proposes withdrawal of low blood pressure drug [press release]. August 16, 2010. TheHeart.org. Retrieved 1 April 2011. .

[3] Midodrine (ProAmatine, generic) Proposed Market Withdrawal – Update September 10, 2010.

[4] Shire Announces Update on ProAmatime September 27, 2011.

[pmid15082846-5] Naschitz J, Dreyfuss D, Yeshurun D, Rosner I (April 2004). "Midodrine treatment for chronic fatigue syndrome". Postgrad Med J 80 (942): 230–2. doi:10.1136/pgmj.2003.011429. PMC 1742969. PMID 15082846.

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midodrine