Clevidipine; Uses, Dosage, Side effects, Interactions Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option. Clevidipine is a dihydropyridine calcium channel blocker indicated for the reduction of blood pressure when oral therapy is not feasible or not desirable. Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option. Mechanism of Action of Clevidipine Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. Indications of Clevidipine High Blood Pressure (Hypertension) Hypertensive Emergency Angina pectoris prophylaxis Raynaud’s Syndrome Heart failure Angina pectoris prophylaxis Contra-Indications of Clevidipine Severe heart failure Abnormally low blood pressure Kidney disease with a reduction in kidney function Fluid Retention in the Legs, arms or hands Blood Circulation Failure due to Serious Heart Condition Chronic idiopathic constipation The high amount of triglyceride in the blood Excessive fat in the blood Severe Narrowing of the Aortic Heart valve Acute Inflammation of the pancreas Fast heartbeat Minimal Change glomerulonephritis Stomach or intestine blockage Narrowing of the intestines Decreased motility function of stomach or intestines Dosage of Clevidipine Strengths: 1 mg, 2 mg, 0.5 mg/mL Hypertension Initial dose: IV infusion of 1 to 2 mg/hour (2 to 4 mL/hour) Dose titration: Dose may be doubled at short (90 seconds) intervals initially. As blood pressure approaches the goal, increase in doses should be less than doubling and intervals between dose adjustments should increase to every 5 to 10 minutes. An increase of approximately 1 to 2 mg/hour generally produces an additional 2 to 4 mmHg decrease in systolic pressure. Maintenance dose: The desired therapeutic response for most patients occurs at doses of 4 to 6 mg/hour (8 to 12 mL/hour). Patients with severe hypertension may require doses up to 32 mg/hour (64 mL/hour). Maximum dose: Most patients were treated with maximum doses of 16 mg/hour (32 mL/hour) or less; however, there is limited short-term experience with doses up to 32 mg/hour (64 mL/hour). Due to lipid load restrictions, no more than 1000 mL (or an average of 21 mg/hour) of clevidipine infusion is recommended per 24 hour period. There is little experience with infusion durations beyond 72 hours at any dose. Side Effects of Clevidipine The most common a severe headache, rapid heartbeat, stiffness in your neck, chest pain, fast or slow heart rate; swelling, rapid weight gain; Xerostomia (dry mouth) A headache Fatigue Skin reactions Hypotension Anxiety Constipation Nausea/vomiting Weight gain/loss Erectile dysfunction More common Abdominal or stomach pain, discomfort, or tenderness chills or fever difficulty with moving a headache, severe and throbbing joint or back pain muscle aching or cramping muscle pains or stiffness chest pressure or squeezing pain in the chest discomfort in arms, shoulders, neck or upper back excessive sweating feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis sudden tingling or coldness in an arm or leg sudden slow or difficult speech sudden drowsiness or need to sleep fast breathing sharp pain when taking a deep breath fast or slow heartbeat coughing up blood rust colored urine decreased amount of urine Rare Anxiety change in vision chest pain or tightness confusion a cough Agitation arm, back, or jaw pain blurred vision chest pain or discomfort convulsions extra heartbeats fainting hallucinations a headache irritability lightheadedness mood or mental changes muscle pain or cramps muscle spasm or jerking of all extremities nervousness Drug Interactions of Clevidipine Clevidipine may interact with the following drugs, supplements, & may change the efficacy of the drug alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin) alpha agonists (e.g., clonidine, methyldopa) angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan) antidiabetes medications (e.g., insulin, metformin, glyburide) atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone) azathioprine barbiturates (e.g., butalbital, pentobarbital phenobarbital) beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol) “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole) calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil) canagliflozin ciprofloxacin calcium supplements (e.g., calcium carbonate, calcium citrate) carbamazepine clopidogrel cyclosporine diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene) duloxetine “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin) guanfacine heparin levodopa medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium) metformin nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen) other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril, ramipril) pentoxifylline macrolide antibiotics (e.g., clarithromycin, erythromycin) methylphenidate monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine) phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil) pregabalin sodium phosphates tizanidine trimethoprim valproic acid warfarin Pregnancy Category FDA Pregnancy Category C Pregnancy This medication should not be taken by women who are or may become pregnant, as clevidipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately. Lactation This medication should not be taken by women who are breastfeeding. The safety and effectiveness of using this medication have not been established for children. References https://www.drugs.com/cdi/clevidipine.html DailyMed https://dailymed.nlm.nih.gov/dailymed/search.cfm?labeltype=all&query=CLEVIDIPINE https://www.webmd.com/drugs/2/drug-151180/clevidipine-intravenous/details/list-contraindications https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022156s003lbl.pdf DrugBank http://www.drugbank.ca/drugs/DB04920#enzymes http://www.drugbank.ca/drugs/DB04920#targetshttp://www.drugbank.ca/drugs/DB04920 EPA DSStox https://comptox.epa.gov/dashboard/dsstoxdb/results?search=DTXSID6057661 European Chemicals Agency – ECHA https://www.echa.europa.eu/web/guest/information-on-chemicals/cl-inventory-database/-/discli/details/254111 FDA Orange Book https://www.fda.gov/Drugs/InformationOnDrugs/ucm129662.htm MassBank of North America (MoNA) http://mona.fiehnlab.ucdavis.edu/spectra/browse?inchikey=KPBZROQVTHLCDU-UHFFFAOYSA-N PubMed Health http://www.ncbi.nlm.nih.gov/pubmedhealth/PMHT0009648/ Springer Nature Read more … WHO ATC https://www.whocc.no/atc/ https://www.whocc.no/atc_ddd_index/ Wikipedia https://en.wikipedia.org/wiki/Clevidipine https://pubchem.ncbi.nlm.nih.gov MeSH https://www.ncbi.nlm.nih.gov/mesh/67118563 http://www.nlm.nih.gov/mesh/meshhome.html https://www.ncbi.nlm.nih.gov/mesh/68002121 ChEBI http://www.ebi.ac.uk/chebi/userManualForward.do#ChEBI%20Ontology Show More