DOCSLIB.ORG

Dihydropyridine Calcium Channel Blockers and Peripheral Side Effects

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Dihydropyridine Calcium Channel Blockers and Peripheral Side Effects Journal of Human Hypertension (2001) 15, 745–746 2001 Nature Publishing Group All rights reserved 0950-9240/01 $15.00 www.nature.com/jhh CASE REPORT Dihydropyridine calcium channel blockers and peripheral side effects A Sirker, CG Missouris and GA MacGregor Blood Pressure Unit, Department of Medicine, St Georges Hospital Medical School, Cranmer Terrace, London SW17 ORE, UK Keywords: dihydropyridine; calcium channel blockers Case report Discussion A 56 year old Caucasian man was referred to our Non-pitting peripheral oedema is one of the most unit in 1994 with a 3-year history of elevated blood commonly described adverse effects of calcium pressure. Six months previously he had been treated channel blocking drugs. It has been described with by his general practitioner with nifedipine tablets all the available dihydropyridine agents and may (Adalat Retard) 10 mg t.d.s. On examination, the occur with diltiazem. An early study suggested that mean supine blood pressure was 135/77 mm Hg. He the incidence of oedema with nifedipine was 11.6% had marked bilateral ankle swelling, hyperpigment- in those treated for 6 months or longer.1 In the more ation of the legs with a petechial, non-blanching recent MATH2 and EXACT3 trials, involving nifedi- rash and areas of erythema which had developed pine in the extended-release formulation (Adalat since starting nifedipine (Figure 1). Nifedipine was XL) for treatment of hypertension, the incidence of discontinued and when he was reviewed in the oedema was 7.7% and 8.1% in those treated for over Blood Pressure Unit 6 weeks later the oedema and 18 and 20 weeks respectively. With amlodipine, an the macular rash had completely resolved; the blood early analysis of pooled data on 581 treated patients pressure was 143/72 mm Hg on non-pharmacologi- found that the incidence of oedema was 11.6% in cal therapy. younger patients and 16.4% in older patients.4 Pre- scription-Event Monitoring (PEM), a national scheme for postmarketing surveillance, has reported that the incidence of peripheral oedema was less with diltiazem than with amlodipine use.5 The peripheral oedema caused by calcium chan- nel blockers is dose dependent3 and is increased by prolonged dependency. The oedema is caused by the inhibition of the pre-capillary reflex6 on standing upright, which increases the hydrostatic pressure on the arteriolar side of the capillary bed leading to an increase in capillary filtration pressure. The oedema is not associated with salt and water retention, indeed the dihydropyridines are natriuretic, and does not improve with diuretic therapy.7 Mild oedema which is not troublesome to the patient does not require specific treatment and may Figure 1 Marked bilateral ankle swelling, associated with a pet- improve with time. In more severe cases, dose 8 echial non-blanching rash and areas of erythema in a patient on reduction or drug withdrawal may be necessary. If treatment with nifedipine tablets (Adalat Retard). continued use of the drug is necessary, for example because of intolerance of other classes of antihyper- tensive, problematic oedema may also be helped by Correspondence: Dr CG Missouris, Blood Pressure Unit, Depart- ment of Medicine, St Georges Hospital Medical School, Cranmer simple measures such as elevation of the legs when Terrace, London SW17 ORE, UK. Fax: 0208 725 2959 seated or lying flat and by wearing graduated com- Received and accepted 27 December 2000 pression stockings. Dihydropyridine calcium channel blockers A Sirker et al 746 A much less recognised but in our experience a 3 Toal CB et al. Nifedipine gastrointestinal therapeutic common associated feature is lower limb petechial, system for hypertensive patients in a primary care set- non-blanching rash. This is believed to result from ting: results of Extended Release Adalat Canadian Trial leakage of red blood cells from capillaries into the (EXACT). Clin Ther 1997; 19: 924–935. interstitium and can cause a long lasting discolour- 4 Osterloh I. The safety of amlodipine. Am Heart J 1989; ation. Our experience, as in this patient, is that with- 118: 1114–1120. 5 Kubota K, Pearce GL, Inman WHW. Vasodilation- drawal of drug results eventually in resolution of related adverse events in diltiazem and dihydropyrid- the rash. ine calcium antagonsists studied by prescription-event monitoring. Eur J Clin Pharmacol 1995; 48:1–7. References 6 Salmasi A-M, Belcaro G, Nicolaides AN. Impaired 1 Terry RW. Nifedipine and therapy in angina pectoris: venoarteriolar reflex as a possible cause for nifedipine- evaluation of safety and side-effects. Am Heart J 1982; induced ankle oedema. Int J Cardiol 1991; 30: 303– 104: 681–689. 307. 2 Krakoff LR, Bravo EL, Tuck ML and the Modern 7 Opie LH. Fluid retention with nifedipine in antihyper- Approach to the Treatment of Hypertension (MATH) tensive therapy. Lancet 1986; 2: 1456. Study Group. Nifedipine gastrointestinal therapeutic 8 Maclean D, MacConnachie AM. Selected side-effects: system in the treatment of hypertension: results of a 1. peripheral oedema with dihyfropyridine calcium multicentre trial. Am J Hypertens 1990; 3: 3185–3255. antagonists. Presc J 1991; 31:4–6. Journal of Human Hypertension.
Load more

Recommended publications
  • Association of Hypertensive Status and Its Drug Treatment with Lipid and Haemostatic Factors in Middle-Aged Men: the PRIME Study
    Journal of Human Hypertension (2000) 14, 511–518 2000 Macmillan Publishers Ltd All rights reserved 0950-9240/00 $15.00 www.nature.com/jhh ORIGINAL ARTICLE Association of hypertensive status and its drug treatment with lipid and haemostatic factors in middle-aged men: the PRIME Study P Marques-Vidal1, M Montaye2, B Haas3, A Bingham4, A Evans5, I Juhan-Vague6, J Ferrie`res1, G Luc2, P Amouyel2, D Arveiler3, D McMaster5, JB Ruidavets1, J-M Bard2, PY Scarabin4 and P Ducimetie`re4 1INSERM U518, Faculte´ de Me´decine Purpan, Toulouse, France; 2MONICA-Lille, Institut Pasteur de Lille, Lille, France; 3MONICA-Strasbourg, Laboratoire d’Epide´miologie et de Sante´ Publique, Strasbourg, France; 4INSERM U258, Hoˆ pital Broussais, Paris, France; 5Belfast-MONICA, Department of Epidemiology, The Queen’s University of Belfast, UK; 6Laboratory of Haematology, La Timone Hospital, Marseille, France Aims: To assess the association of hypertensive status this effect remained after multivariate adjustment. Cal- and antihypertensive drug treatment with lipid and hae- cium channel blockers decreased total cholesterol and mostatic levels in middle-aged men. apoproteins A-I and B; those differences remained sig- Methods and results: Hypertensive status, antihyperten- nificant after multivariate adjustment. ACE inhibitors sive drug treatment, total and high-density lipoprotein decreased total cholesterol, triglycerides, apoprotein B (HDL) cholesterol, triglyceride, apoproteins A-I and B, and LpE:B; and this effect remained after multivariate lipoparticles LpA-I,
    [Show full text]
  • Sharon R. Roseman, MD, FACP Practice Limited to Gastroenterology
    Sharon R. Roseman, MD, FACP Practice Limited to Gastroenterology 701 Broad Street, Suite 411 Sewickley, PA 15143 (412) 749-7160 Fax: (412) 749-7388 http://www.heritagevalley.org/sharonrosemanmd Patient Drug Education for Diltiazem / Nifedipine Ointment Diltiazem/Nifedipine ointment is used to help heal anal fissures. The ointment relaxes the smooth muscle around the anus and promotes blood flow which helps heal the fissure (tear). The ointment reduces anal canal pressure, which diminishes pain and spasm. We use a diluted concentration of Diltiazem/Nifedipine compared to what is typically used for heart patients, and this is why you need to obtain the medication from a pharmacy which will compound your prescription. It is also prescribed to treat anal sphincter spasm, painful hemorrhoids and pelvic floor spasm. The Diltiazem/Nifedipine ointment should be applied 3 times per day, or as directed. A pea-sized drop should be placed on the tip of your finger and then gently placed inside the anus. The finger should be inserted 1/3 – 1/2 its length and may be covered with a plastic glove or finger cot. You may use Vaseline ® to help coat the finger or dilute the ointment. (If you are unable or hesitant to use your finger to administer the ointment TELL U S and we will order you a suppository to use as an “applicator”.) If you are advised to mix the Diltiazem/Nifedipine with steroid ointment, limit the steroids to one to two weeks. The first few applications should be taken lying down, as mild light- headedness or a brief headache may occur.
    [Show full text]
  • Valproate-Olanzapine-Nifedipine Interaction Related Pedal Edema
    Letter-to-the Editor Taiwanese Journal of Psychiatry (Taipei) Vol. 28 No. 3 2014 • 181 • Valproate-olanzapine-nifedipine Interaction Related Pedal Edema Patient’s bilateral pedal pitting edema did not Case Report resolve spontaneously after discontinuing olan- zapine until he received diuretics with furosemide A 45-year-old single male patient with bipo- 40 mg/day and spironolactone 75 mg/day on the lar I disorder was admitted to acute ward of our 21st day of pitting edema. He required further hospital due to depressive mood with irritability treatment, and had normal fi ndings in physical ex- for more than one month. The fi nding of physical amination and repeated laboratory tests. examination at admission revealed no bilateral pedal edema under long-term usage of valproate Comment 700 mg/day as mood stabilizer, nifedipine 30 mg/ day for essential hypertension, and allopurinol There have been some clinical reports to as- 100 mg/day for gouty arthritis before hospitaliza- sociate olanzapine treatment with bilateral lower tion. The results of laboratory tests for electro- extremity edema since 2000 [1]. Pre-clinical trials lytes, renal function, liver function, chest X-ray, of oral olanzapine (doses being equal or greater and electrocardiography were also within normal than 2.5 mg/day) have also reported peripheral limits. edema as a rare adverse event. The pathophysio- During this hospitalization, we added olan- logical mechanism of low extremity edema re- zapine 5 mg/day to control manic symptoms. Five mains unknown, although some mechanisms days later, he reported bilateral swelling over low- could be proposed, such as olanzapine’s blockage er legs and ankles, a bilateral 2+ pitting edema in of α1, M1, M3 and 5-HT2 receptors [2, 3].
    [Show full text]
  • Nifedipine Adalat, Adalat PA, Adalat XL, Apo-Nifed, Nu-Nifed
    Nifedipine Adalat, Adalat PA, Adalat XL, Apo-Nifed, Nu-Nifed Information for patients and families Why am I taking this drug? Nifedipine helps to: Control high blood pressure (hypertension) Reduce how often you have chest pains (angina) How does nifedipine work? Nifedipine belongs to a class of drugs called calcium channel blockers. It relaxes the muscles in your blood vessels so that they will open wider. This lowers your blood pressure and makes it easier for your heart to pump blood. Nifedipine also opens the blood vessels in your heart (coronary arteries) wider so that more blood and oxygen can get to the heart muscle. This is helpful for angina, which happens when the heart muscle is not getting enough blood and oxygen for the amount of work it is doing. How should I take this medicine? Never chew or crush nifedipine tablets. It is best to take nifedipine on an empty stomach. Avoid taking it with grapefruit juice. Take your pills at the same time every day. Do not stop taking this drug unless you check with your doctor first. You may need to gradually take less and less instead of stopping all at once. What should I do if I miss a dose? If you are late taking a dose and it is almost time for the next one, skip the late dose then follow your regular schedule. Never take more than 1 dose at a time. If you do not know what to do, ask your pharmacist, doctor or nurse practitioner. What should I expect from this medicine? Nifedipine usually starts to work within 30 to 60 minutes after you take it.
    [Show full text]
  • Print This Article
    Print ISSN: 2319-2003 | Online ISSN: 2279-0780 IJBCP International Journal of Basic & Clinical Pharmacology DOI: http://dx.doi.org/10.18203/2319-2003.ijbcp20174634 Original Research Article Anticonvulsant effect of nifedipine, dizepam and in combination on pentylenetetrazol induced experimental models of epilepsy on albino rats Muralidhar C.1, Vijay Prasad S.2*, Sridhar I.3 ABSTRACT Background: In many patients, the presently available antiepileptic drugs such 1Medical Officer, Under as phenobarbital, phenytoin, benzodiazepines, sodium valproate, etc., are unable DMHO, Medak, Telangana, to control seizures efficiently and the problem of adverse effects has also not been India circumvented completely and approximately 30% of the patients continue to have 2Department of Pharmacology, seizures with current antiepileptic drugs therapy. Hence, search should continue Dr Vithalrao Vikhe Patil to develop newer, more effective, and safer neuro-protective agents for treatment Foundation's Medical College, of epilepsy. Aim of the study was to investigate the activity of nifedipine, the Ahmednagar, Maharashtra, dihydropyridine calcium channel blocker, diazepam, the benzodiazepine anti- India convulsant of established efficacy and their combinations against rat models of 3Department of Pharmacology, pentylenetetrazol (PTZ) induced convulsions. Method: Wister albino rats of Government Medical College, either sex, weighing between 150-220gm were used. Rats were divided into 10 Nizamabad, Telangana, India groups, in each group n=6 total N=60. Methods: PTZ was administration 30 min after test drug administration. Received: 17 September 2017 Intraperitoneal injection of PTZ at the dose of 80mg/Kg body weight were Accepted: 22 September 2017 administered to the rats to produce chemically-induced seizure. The effect of nifedipine and diazepam were assessed on such seizure model.
    [Show full text]
  • In Vitro Study of the Effect of Nifedipine on Human Fibroblasts
    applied sciences Article Biology of Drug-Induced Gingival Hyperplasia: In Vitro Study of the Effect of Nifedipine on Human Fibroblasts Dorina Lauritano 1,*,† , Giulia Moreo 1,†, Fedora Della Vella 2 , Annalisa Palmieri 3, Francesco Carinci 4 and Massimo Petruzzi 2 1 Centre of Neuroscience of Milan, Department of Medicine and Surgery, University of Milano-Bicocca, 20126 Milan, Italy; [email protected] 2 Interdisciplinary Department of Medicine, University of Bari, 70121 Bari, Italy; [email protected] (F.D.V.); [email protected] (M.P.) 3 Department of Experimental, Diagnostic and Specialty Medicine, University of Bologna, Via Belmoro 8, 40126 Bologna, Italy; [email protected] 4 Department of Translational Medicine, University of Ferrara, 44121 Ferrara, Italy; [email protected] * Correspondence: [email protected] † These authors contribute equally to this work. Abstract: Background: It has been proven that the antihypertensive agent nifedipine can cause gingi- val overgrowth as a side effect. The aim of this study was to analyze the effects of pharmacological treatment with nifedipine on human gingival fibroblasts activity, investigating the possible patho- genetic mechanisms that lead to the onset of gingival enlargement. Methods: The expression profile of 57 genes belonging to the “Extracellular Matrix and Adhesion Molecules” pathway, fibroblasts’ viability at different drug concentrations, and E-cadherin levels in treated fibroblasts were assessed using real-time Polymerase Chain Reaction, PrestoBlue™ cell viability test, and an enzyme-linked immunoassay (ELISA), respectively. Results: Metalloproteinase 24 and 8 (MMP24, MMP8) showed Citation: Lauritano, D.; Moreo, G.; significant upregulation in treated cells with respect to the control group, and cell adhesion gene Vella, F.D.; Palmieri, A.; Carinci, F.; CDH1 (E-cadherin) levels were recorded as increased in treated fibroblasts using both real-time Petruzzi, M.
    [Show full text]
  • Guideline for Preoperative Medication Management
    Guideline: Preoperative Medication Management Guideline for Preoperative Medication Management Purpose of Guideline: To provide guidance to physicians, advanced practice providers (APPs), pharmacists, and nurses regarding medication management in the preoperative setting. Background: Appropriate perioperative medication management is essential to ensure positive surgical outcomes and prevent medication misadventures.1 Results from a prospective analysis of 1,025 patients admitted to a general surgical unit concluded that patients on at least one medication for a chronic disease are 2.7 times more likely to experience surgical complications compared with those not taking any medications. As the aging population requires more medication use and the availability of various nonprescription medications continues to increase, so does the risk of polypharmacy and the need for perioperative medication guidance.2 There are no well-designed trials to support evidence-based recommendations for perioperative medication management; however, general principles and best practice approaches are available. General considerations for perioperative medication management include a thorough medication history, understanding of the medication pharmacokinetics and potential for withdrawal symptoms, understanding the risks associated with the surgical procedure and the risks of medication discontinuation based on the intended indication. Clinical judgement must be exercised, especially if medication pharmacokinetics are not predictable or there are significant risks associated with inappropriate medication withdrawal (eg, tolerance) or continuation (eg, postsurgical infection).2 Clinical Assessment: Prior to instructing the patient on preoperative medication management, completion of a thorough medication history is recommended – including all information on prescription medications, over-the-counter medications, “as needed” medications, vitamins, supplements, and herbal medications. Allergies should also be verified and documented.
    [Show full text]
  • Substance Abuse
    \1\A-10/PSA/93.10 ORIGINAL: ENGUSH DISTR.: GENERAL PROGRAMME ON SUBSTANCE ABUSE Approaches to Treatment of Substance Abuse WORLD HEALTH ORGANIZATION ABSTRACf The aim of this report is to provide an updated description of different methods used around the world to treat health problems associated with substance use. The scope of treatment approaches currently practised around the world is wide, ranging from traditional healing practices via mutual self-help groups, psychological/behavioural treatment to pharmacological treatment. Also included is a chapter on the generalist responses to alcohol and other drug problems and a chapter on the concept of harm minimization. Another aspect is a chapter on specific descriptors, which distinguishes different treatments from one another and provides economic means of describing them. Social and structural extra-treatment factors influencing the treatment process are also a subject described in this report. ©World Health Organization, 1993 This document is not a formal publication of the World Health Organization (WHO), and all rights are reserved by the Organization. The document may, however, be freely reviewed, abstracted, reproduced and translated in part or in whole, but not for sale nor for use in conjunction with commercial purposes. The views expressed in documents by named authors are solely the responsibility of those authors. ii CONTENTS page Acknowledgements . v Introduction . 1 I. Descriptors of Treatments . 3 11. Factors Influencing Treatment . 31 Ill. Generalist Responses to Alcohol and other Drug Problems . 53 IV. Pharmacological Treatment of Dependence on Alcohol and other Drugs: An Overview . 75 V. Psychological, Behavioural and Psychodynamic Treatments for Substance Abuse . 103 VI.
    [Show full text]
  • World Health Organization Model List of Essential Medicines, 21St List, 2019
    World Health Organizatio n Model List of Essential Medicines 21st List 2019 World Health Organizatio n Model List of Essential Medicines 21st List 2019 WHO/MVP/EMP/IAU/2019.06 © World Health Organization 2019 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. World Health Organization Model List of Essential Medicines, 21st List, 2019. Geneva: World Health Organization; 2019. Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data. CIP data are available at http://apps.who.int/iris.
    [Show full text]
  • Salbutamol Metformin Nifedipine Diclofenac Simvastatin Mefenamic
    Electronic Supplementary Material (ESI) for RSC Advances. This journal is © The Royal Society of Chemistry 2018 Salbutamol Metformin Ibuprofen Acetaminophen Nifedipine Diclofenac Caffeine Simvastatin Mefenamic Acid Perindopril Figure S 1. Chemical structures of the selected pharmacetical Figure S2. TIC chromatogram of a standard mixture of 1 ng μL-1 for targeted compounds analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S3. MRM chromatogram of a standard mixture of 1 ng μL-1 for targeted compounds analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S4. TIC chromatogram of a blank sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S5. MRM chromatogram of a blank sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S6. TIC chromatogram of a tap sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S7. MRM chromatogram of a tap sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S8. TIC chromatogram of an effluent wastewater (EF) sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S9. MRM chromatogram of an effluent wastewater sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S10. TIC chromatogram of an influent wastewater sample (IN) analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S11. MRM chromatogram of an influent wastewater sample analyzed by negative and positive ionization (ESI) modes of UPLC-MS/MS. Figure S12.
    [Show full text]
  • Oral Health Fact Sheet for Dental Professionals Adults with Congenital Cardiac Disorders
    Oral Health Fact Sheet for Dental Professionals Adults with Congenital Cardiac Disorders Congenital cardiac disorders are imperfections or malformations of the heart existing at, and usually before, birth regardless of their causation. (ICD9 code 746.9) Prevalence • Approximately 1% Manifestations Clinical varies with type of congenital defect (e.g. atrial/ventricular septal defects, pulmonary/aortic stenosis, transposition, heart valve abnormalities) • Pulmonary congestion/labored breathing • Heart murmur • Cardiomegaly • Congestive heart failure • Hypoxic spells • Cyanosis • Poor physical development • Clubbing of the terminal phalanges of the fingers Oral • Infective endocarditis risk from dental treatment • Post-operative bleeding risk in patients with anti-coagulated status following surgical procedures • May have oral manifestations caused by co-occurring disorders Other Potential Disorders/Concerns • Depression/Anxiety • Genetic and syndromic conditions (~11%) such as Down, Turner, Marfan and Ehler Danlos syndromes; osteogenesis imperfecta • Asthma • Intellectual disabilities • Esophageal atresia Management Medication The list of medications below are intended to serve only as a guide to facilitate the dental professional’s understanding of medications that can be used for Congenital Cardiac Disorders. Medical protocols can vary for individuals with Congenital Cardiac Disorders from few to multiple medications. MEDICATION TYPE MEDICATION SIDE EFFECTS/DRUG INTERACTIONS ACE inhibitors Benazepril (Lotensin) Cough, low blood pressure,
    [Show full text]
  • Identification of the Hypertension Drug Niflumic Acid As a Glycine Receptor Inhibitor
    www.nature.com/scientificreports OPEN Identifcation of the hypertension drug nifumic acid as a glycine receptor inhibitor Daishi Ito1, Yoshinori Kawazoe2, Ayato Sato3, Motonari Uesugi4 & Hiromi Hirata1* Glycine is one of the major neurotransmitters in the brainstem and the spinal cord. Glycine binds to and activates glycine receptors (GlyRs), increasing Cl− conductance at postsynaptic sites. This glycinergic synaptic transmission contributes to the generation of respiratory rhythm and motor patterns. Strychnine inhibits GlyR by binding to glycine-binding site, while picrotoxin blocks GlyR by binding to the channel pore. We have previously reported that bath application of strychnine to zebrafsh embryos causes bilateral muscle contractions in response to tactile stimulation. To explore the drug-mediated inhibition of GlyRs, we screened a chemical library of ~ 1,000 approved drugs and pharmacologically active molecules by observing touch-evoked response of zebrafsh embryos in the presence of drugs. We found that exposure of zebrafsh embryos to nifedipine (an inhibitor of voltage- gated calcium channel) or nifumic acid (an inhibitor of cyclooxygenase 2) caused bilateral muscle contractions just like strychnine-treated embryos showed. We then assayed strychnine, picrotoxin, nifedipine, and nifumic acid for concentration-dependent inhibition of glycine-mediated currents of GlyRs in oocytes and calculated IC50s. The results indicate that all of them concentration-dependently inhibit GlyR in the order of strychnine > picrotoxin > nifedipine > nifumic acid. Glycine, one of the major neurotransmitters, binds to glycine receptor (GlyR), mediating fast inhibitory synaptic transmission in the brain stem and the spinal cord1,2. Inhibitory glycinergic transmission is involved in generating rhythms such as respiration and walking/running.
    [Show full text]