2016년 12월 16일 금요일

Calcium antagonist

Calcium antagonist

I perform antagonism (inhibition) of a function of the Ca2+ channel in the smooth muscle of the blood vessel, and the calcium antagonist (calcium きっこうざい British: calcium channel blocker, CCB) is a drug indicating the vasodilatation action. Application cases include high blood pressure, angina mainly.

Table of contents

Summary

I bind to the Ca2+ channel on the cell membrane not a drug letting calcium compete for the calcium antagonist and am a drug obstructing the calcium ion inflow in the cell. The name "calcium antagonist" should originally assume it a "Ca2+ channel antagonist" "calcium ion inflow suppressant" not appropriateness, but the name of "the calcium antagonist" becomes common in Japan (it was dose-dependent and controlled blood vessel and the myocardium shrinkage by the Ca ion without understanding action mechanism at the time of development, and the appearance top was listed in calcium with "a calcium antagonist" because it was the action that I competed for). But there is misunderstanding that it is the drug that absorption of calcium is obstructed in a part for this general name.

The calcium antagonists are structurally greatly classified in three. I am used for high blood pressure mainly, and the dihydropyridine system having high blood vessel selectivity is done with a first-line drug of the hypertensive treatment and is used for a wide patient. The vasodilatation action is gentle and quiet, and the benzothiazepine system is relatively weak, but I provide heart rate restraint, and first choice of angina is used because, besides, crown スパズム restraint action is strong. Because restraint action pro-stimulation generation, conduction in phenyl alkylamine system (sinus node, atrioventricular node) is high, I am often used for tachycardiac arrhythmia such as PSVT (発作性上室性頻拍) or the atrial fibrillation. In addition, teratogenic possibility is reported and is contraindicated in a patient with the possibility of a pregnant woman, the pregnancy.

Action mechanism

A large number of subtypes such as L,T,N,P are known to the Ca2+ channel, but it is thought that the commercially available calcium antagonist gets the reactions of drugs activity mainly now by preventing the calcium entry through the L-form Ca2+ channel.

It is thought that the difference in action varies in a binding site to L-form Ca2+ channel. Action to blood vessel is shrinkage restraint action of the blood vessels with the Ca ion inflow restraint to a vascular smooth muscle cell, and the artery with the smooth muscle cell is stronger in shrinkage restraint than a vein. In addition, the expansion action with coronary arteries is higher than peripheral artery artery with the same artery blood vessel. The dihydropyridine calcium antagonist may raise glomerulus internal pressure to expand the afferent arteriole with the kidney, and it is thought that I am inferior to ACE inhibitor as the progress prevention of the nephrosclerosis. A decrease in excitement frequency of the sinoatrial node and the conduction restraint of the atrioventricular node are known to be effective with the heart, but a rise in heart rate may be seen with a pressoreceptor reflection with the vasodilatation action without a blood vessel choice system being high in the dihydropyridine calcium antagonist, and being able to hardly expect the effect at the clinical dose. In addition, valproic acid (デパケン) is an antiepileptic drug acting on Model T Ca2+ channel.

Main side effect

  • By the vasodilatation: Face flush, headache, feeling of heat (hot flashes), lower limbs edema (swelling)
  • By the excessive depression: Low blood pressure (dizziness)
  • By the pro-heart stimulation generation (sinus node), conduction (atrioventricular node) restraint: Bradycardia, bedroom affairs block (verapamil, diltiazem)
  • Unidentified: A gum swelling (medicamentosus gingival hyperplasia) [1]

Classification

Dihydropyridine-based

It is the classification that nifedipine (アダラート) and nicardipine (ペルジピン) and amlodipine (Jin Amuro and norbasque) are included in. The dihydropyridine system binds to the N part (N of Nifedipin) of the L-form Ca2+ channel. I vasodilate it and act, and depression action is strong, and there is little action to myocardium. I am used for high blood pressure and angina well. It is thought that there are few negative inotropic action and antiarrhythmic action. As for nifedipine, action expression is too early, and the rise in heart rate might be recognized, but アダラート L overcomes the problems by assuming it a controlled release agent.

Because アダラートカプセル is not a controlled release agent, in the case of the quick depression in the hypertensive emergency symptom, I am used and was often used because I can get a depression effect in around 20 minutes, but the use is not recommended now

  1. Transfer [hypertensive treatment guidelines [1]]

.

Because nicardipine is available for a stable intravenous drip, I am liked in the ward. 1 ampoule of ペルジピン is 10 mg/10 mL. I do not use it straight and use it according to the attached document in diluted form by all means. Because a maintenance dose is 2-10 γ, 1 γ is equivalent to 3 mL/hr with an undiluted solution if the weight is 50kg. It starts from undiluted solution 2 mL/hr and it supports scaling and often maintains it in the range of 2-20 mL/hr. It is passable to start from a low dose called 1.5 mL/hr which is 0.5 γ when I am complicated with heart failure because a side effect includes tachycardiac arrhythmia. In addition, the patient that hemostasis is not completed in the cerebral hemorrhage immediate nature period is contraindicated to use.

Like a list of following dihydropyridine drugs released to date, there is "a dipin" in the end of the generic name by all means.

Benzothiazepine-based

Diltiazem (ヘルベッサー) is included. Diltiazem binds to the D part (D of diltiazem) of the L-form Ca2+ channel. It is different from the V (V of verapamil) part where dihydropyridine-based connected N part and verapamil bind to, and this is connected in a difference of the action. In addition, I inhibit a bond with verapamil whereas I increase the bond of each other's drugs with the dihydropyridine.

I act on blood vessel (depression) of the erasion to blood vessel (big coronary expansion, antiスパズム) of the heart. But it is first choice for angina of the normal blood pressure because the normal blood pressure does not lower the depression action in mild. When there is the anginal attack for angina of crown スパズム characteristics early in the morning, I give 100-200 mg orally before after dinner or going to bed. The patient that a case and angina and myocardium ischemia in hope of mild depression, bradycardia action are doubted is given 100-200 mg a day orally for the high blood pressure.

10 mg, 50 mg, three drugs type of 250 mg are to the ヘルベッサー injection agent. As for the restraint of the bedroom affairs missionary work, the action of bradycardia, the gentle and quiet bolus dosage of the verapamil injection is used mainly, and, as for the diltiazem injection, there is much use by the continuation intravenous feeding intravenous administration at the time of hypertensive emergency symptom and unstable angina without being used in this country too much.

I dissolve 5% of 10 mg of component preparation in grape sugar solution 10mL for tachycardiac arrhythmia such as PSVT and do 靜注 in three minutes. I last for unstable angina and a hypertensive emergency symptom and am administered intravenously and am maintained in 1-5 γ for unstable angina in 5-15 γ for the hypertensive emergency symptom. When the usage dissolves 50 mg agent type 3A with 100 ml of 5% grape sugar solutions, it is 1.5 mg/mL. It is 1 γ dosage when I give it in 2 mL/hr because 1 γ becomes 3 mg/hr when the weight is 50 kg.

Benzothiazepine system and the benzodiazepine system of the minor tranquilizer are attention in a name being similar, but being totally different.

Phenyl alkylamine system

Verapamil (ワソラン) is included. Verapamil binds to the V part of the L-form Ca2+ channel. An effect becomes a cause to fall when I use it together because it falls on the D part where diltiazem binds to. I act on both heart and blood vessel, but the action to heart is predominantly in comparison with diltiazem strong.

I am used for atrial fibrillation, rate control of the atrial flutter and a stop of PSVT. Because the depression effect is seen, monitoring of the blood pressure is important by the stop of PSVT. I assume ワソラン 5 mg 10mL with a 5% grape sugar solution in PSVT and administer 4mL (2 mg) intravenously and add by 2mL (1 mg) two minutes later while seeing blood pressure, an electrocardiogram. The gross weight prevents you from exceeding 10 mg. In addition, a right leg block, the left axes shift type ventricular tachycardia are said to be verapamil 感受性特発性心室頻拍, and verapamil is effective.

Other

There is bepridil (ベプリコール). It is a multichannel blocker, and this may be used as antiarrhythmic.

Interaction

Food

When I eat specific food during remedy to a calcium antagonist, a phenomenon (interaction) to more strongly show the action of the drug is known [2]. This phenomenon is reported a lot with a drug metabolized with CYP3A4 functioning as (detoxification enzyme). With the report that the possibility that wake up interaction by flavonoids in fruit juice liquid inhibiting small molecule excretion pump mechanism to be seen in an intestinal mucosa epithelium cell other than above-mentioned CYP3A4 as a cause of the interaction suggests [3]. In the body, a phenomenon to say, "blood pressure decreases too much by the resolution of the medicine being suppressed, and the blood concentration of the drug rising" happens. Therefore, with furanocoumarin having CYP3A4 activity inhibition action-rich grape fruit juice, a shaddock, shaddock, the Chinese citron let drink, and should not generally perform it. The interaction does not happen with Wenzhou mandarin orange, the orange juice with the same citrus fruits either. But, with some drugs including amlodipine that influence of the liver first pass effect is small, there is known to be relatively little influence of the CYP3A4 activity inhibition action with the grapefruit juice.

Drug

By a Canadian researcher, blood concentration increases by the erythromycin of the macrolide derivative antibiotic, combination with the clarithromycin, and possibility to cause the shock of low blood pressure and the dangerous level like grapefruit fruit juice has it pointed out [4]; [5].

Product commercially available now

Footnote

  1. ^ Kazuyuki Noguchi, Toshiaki Nakamura, innocence Yoshinori: Diagnosis and treatment Japan conservative dentistry magazine Vol.57 (2014) No. 6 p.477-483 of special periodontal disease
  2. ^ 植沢芳広 (2008). "QSAR analysis of the interaction between grapefruit juice - drug." Chemical Society of Japan computerization department bulletin 26:114. NAID 130000091003. JOI:JST.JSTAGE/cicsj/26.114. 
  3. ^ high long eyes, Ayako Onishi, Junko Uchida, Shiho Yamada, citizen of Hiroshi Matsuo, Satoshi Morimoto, Shozan Masahiro, Yasufumi Sawada (1998). "Effects such as the grapefruit juice which gives it to the function of the P glycoprotein in the gastrointestinal absorption of the drug." Pharmacokinetics 13 (No.supplement): 110-111. doi: 10.2133/dmpk.13.supplement_110. NAID 10007629682. 
  4. ^ Wright AJ, Gomes T, Mamdani MM, Horn JR, Juurlink DN (2011). "The risk of hypotension following co-prescription of macrolide antibiotics and calcium-channel blockers". CMAJ 183 (3). doi: 10.1503/cmaj.100702. PMC 3042440. It is http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=3042440. PMID 21242274 
  5. ^ smart smart healthy NIKKEI NET (January 27, 2011). "The combination of some antibiotics and calcium antagonist brings low blood pressure". March 8, 2011 reading.

References

  • For Mamoru Sakakibara, Junichi Taguchi "circulatory organ internal medicine Golden handbook" 南江堂, 2,008 years, it is the revision second edition. ISBN 9784524243860。
  • Yuji Murakawa "circulatory organ therapeutic drug file" medical science international, 2003. ISBN 978-4,895,922,951。
  • Norio Taira (1989). "The action mechanism of the calcium antagonist." Pharmacokinetics 4 (3): 247-247. doi: 10.2133/dmpk.4.247. 
  • 山中教造, Makoto Suzuki, sect lotus Shiro, Junnichi Ishikawa (1991). "Depression action of new Ca antagonist Amlodipine besilate." Japanese pharmacologic magazine 97 (2): 115-126. doi: 10.1254/fpj.97.2_115. 

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