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| Mechanism of Action |
Epinephrine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Epinephrine works via the stimulation of alpha and beta-1 adrenergic receptors, and a moderate activity at beta-2 adrenergic receptors.
Lidocaine¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action.
|
| Pharmacology |
Epinephrine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Epinephrine is indicated for intravenous injection in treatment of acute hypersensitivity, treatment of acute asthmatic attacks to relieve bronchospasm, and treatment and prophylaxis of cardiac arrest and attacks of transitory atrioventricular heart block with syncopal seizures (Stokes-Adams Syndrome). The actions of epinephrine resemble the effects of stimulation of adrenergic nerves. To a variable degree it acts on both alpha and beta receptor sites of sympathetic effector cells. Its most prominent actions are on the beta receptors of the heart, vascular and other smooth muscle. When given by rapid intravenous injection, it produces a rapid rise in blood pressure, mainly systolic, by (1) direct stimulation of cardiac muscle which increases the strength of ventricular contraction, (2) increasing the heart rate and (3) constriction of the arterioles in the skin, mucosa and splanchnic areas of the circulation. When given by slow intravenous injection, epinephrine usually produces only a moderate rise in systolic and a fall in diastolic pressure. Although some increase in pulse pressure occurs, there is usually no great elevation in mean blood pressure. Accordingly, the compensatory reflex mechanisms that come into play with a pronounced increase in blood pressure do not antagonize the direct cardiac actions of epinephrine as much as with catecholamines that have a predominant action on alpha receptors.
Lidocaine¿¡ ´ëÇÑ Pharmacology Á¤º¸ Lidocaine is an anesthetic agent indicated for production of local or regional anesthesia and in the treatment of ventricular tachycardia occurring during cardiac manipulation, such as surgery or catheterization, or which may occur during acute myocardial infarction, digitalis toxicity, or other cardiac diseases. The mode of action of the antiarrhythmic effect of Lidocaine appears to be similar to that of procaine, procainamide and quinidine. Ventricular excitability is depressed and the stimulation threshold of the ventricle is increased during diastole. The sinoatrial node is, however, unaffected. In contrast to the latter 3 drugs, Lidocaine in therapeutic doses does not produce a significant decrease in arterial pressure or in cardiac contractile force. In larger doses, lidocaine may produce circulatory depression, but the magnitude of the change is less than that found with comparable doses of procainamide.
|
| Metabolism |
Epinephrine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available
Lidocaine¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6)
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| Protein Binding |
Lidocaine¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 60-80%
|
| Half-life |
Epinephrine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 minutes
Lidocaine¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 109 minutes
|
| Absorption |
Epinephrine¿¡ ´ëÇÑ Absorption Á¤º¸ Usually this vasodilator effect of the drug on the circulation predominates so that the modest rise in systolic pressure which follows slow injection or absorption is mainly the result of direct cardiac stimulation and increase in cardiac output.
Lidocaine¿¡ ´ëÇÑ Absorption Á¤º¸ Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
|
| Biotransformation |
Epinephrine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Epinephrine is rapidly inactivated in the body and is degraded by enzymes in the liver and other tissues. The larger portion of injected doses is excreted in the urine as inactivated compounds and the remainder either partly unchanged or conjugated. The drug becomes fixed in the tissues and is inactivated chiefly by enzymatic transformation to metanephrine or normetanephrine either of which is subsequently conjugated and excreted in the urine in the form of sulfates and glucuronides. Either sequence results in the formation of 3-methoxy-4-hydroxy-mandelic acid which also is detectable in the urine.
Lidocaine¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic.
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| Toxicity |
Epinephrine¿¡ ´ëÇÑ Toxicity Á¤º¸ Skin, LD50 = 62 mg/kg (rat)
Lidocaine¿¡ ´ëÇÑ Toxicity Á¤º¸ The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
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| Drug Interactions |
Epinephrine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Acebutolol Hypertension, then bradycardiaAlseroxylon Increased arterial pressureAmitriptyline The tricyclic increases the sympathomimetic effectAmoxapine The tricyclic increases the sympathomimetic effectAtenolol Hypertension, then bradycardiaBetaxolol Hypertension, then bradycardiaBevantolol Hypertension, then bradycardiaBisoprolol Hypertension, then bradycardiaCarteolol Hypertension, then bradycardiaCarvedilol Hypertension, then bradycardiaClomipramine The tricyclic increases the sympathomimetic effectDesipramine The tricyclic increases the sympathomimetic effectDeserpidine Increased arterial pressureDoxepin The tricyclic increases the sympathomimetic effectEntacapone Entacapone increases the effect and toxicity of sympathomimeticsMethylergonovine Possible marked increase of arterial pressureNortriptyline The tricyclic increases the sympathomimetic effectProtriptyline The tricyclic increases the sympathomimetic effectImipramine The tricyclic increases the sympathomimetic effectEsmolol Hypertension, then bradycardiaGuanethidine The agent decreases the effect of guanethidineIsocarboxazid Increased arterial pressureLabetalol Hypertension, then bradycardiaLinezolid Possible increase of arterial pressureMethyldopa Increased arterial pressureMetoprolol Hypertension, then bradycardiaMidodrine Increased arterial pressureMoclobemide Moclobemide increases the sympathomimetic effectNadolol Hypertension, then bradycardiaPenbutolol Hypertension, then bradycardiaOxytocin Possible marked increase of arterial pressurePhenelzine Increased arterial pressurePindolol Hypertension, then bradycardiaPractolol Hypertension, then bradycardiaPropranolol Hypertension, then bradycardiaRasagiline Increased arterial pressureReserpine Increased arterial pressureSotalol Hypertension, then bradycardiaTimolol Hypertension, then bradycardiaTranylcypromine Increased arterial pressureTrimipramine The tricyclic increases the sympathomimetic effectErgonovine Possible marked increase of arterial pressureOxprenolol Hypertension, then bradycardiaPargyline Increased arterial pressure
Lidocaine¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸]
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| Food Interaction |
Lidocaine¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
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| Drug Target |
[Drug Target]
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| Description |
Epinephrine¿¡ ´ëÇÑ Description Á¤º¸ The active sympathomimetic hormone from the adrenal medulla in most species. It stimulates both the alpha- and beta- adrenergic systems, causes systemic vasoconstriction and gastrointestinal relaxation, stimulates the heart, and dilates bronchi and cerebral vessels. It is used in asthma and cardiac failure and to delay absorption of local anesthetics. [PubChem]
Lidocaine¿¡ ´ëÇÑ Description Á¤º¸ A local anesthetic and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]
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| Dosage Form |
Epinephrine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularLiquid OralSolution IntramuscularSolution IntravenousSolution NasalSolution Respiratory (inhalation)Solution / drops OphthalmicSolution / drops Oral
Lidocaine¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Aerosol TopicalAerosol, metered TopicalCream TopicalGel TopicalJelly TopicalJelly UrethralLiquid BuccalLiquid DentalLiquid InfiltrationLiquid IntravenousLiquid OralLiquid TopicalLotion TopicalOintment TopicalSolution InfiltrationSolution IntramuscularSolution IntravenousSolution OralSolution TopicalSpray TopicalSwab Topical
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| Drug Category |
Epinephrine¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic AgonistsAdrenergic alpha-AgonistsAdrenergic beta-AgonistsBronchodilator AgentsMydriaticsSympathomimeticsVasoconstrictor Agents
Lidocaine¿¡ ´ëÇÑ Drug_Category Á¤º¸ AnestheticsAnesthetics, LocalAnti-Arrhythmia AgentsAntiarrhythmic Agents
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| Smiles String Canonical |
Epinephrine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CNCC(O)C1=CC(O)=C(O)C=C1
Lidocaine¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
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| Smiles String Isomeric |
Epinephrine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CNC[C@H](O)C1=CC(O)=C(O)C=C1
Lidocaine¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CCN(CC)CC(=O)NC1=C(C)C=CC=C1C
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| InChI Identifier |
Epinephrine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C9H13NO3/c1-10-5-9(13)6-2-3-7(11)8(12)4-6/h2-4,9-13H,5H2,1H3/t9-/m0/s1
Lidocaine¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C14H22N2O/c1-5-16(6-2)10-13(17)15-14-11(3)8-7-9-12(14)4/h7-9H,5-6,10H2,1-4H3,(H,15,17)/f/h15H
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| Chemical IUPAC Name |
Epinephrine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 4-[(1R)-1-hydroxy-2-methylaminoethyl]benzene-1,2-diol
Lidocaine¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 2-diethylamino-N-(2,6-dimethylphenyl)acetamide
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| Drug-Induced Toxicity Related Proteins |
DOCA ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Aquaporin-2 Drug:DOCA Toxicity:hypertension. [¹Ù·Î°¡±â] EPINEPHRINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Interleukin-8 Drug:epinephrine Toxicity:inflammation. [¹Ù·Î°¡±â] Replated Protein:Leptin Drug:epinephrine Toxicity:epinephrine-induced suppression in human obesity. [¹Ù·Î°¡±â] Replated Protein:Glutathione reductase Drug:epinephrine Toxicity:cytotoxic. [¹Ù·Î°¡±â] Replated Protein:Alpha-2A adrenergic receptor Drug:epinephrine Toxicity:platelet aggregation. [¹Ù·Î°¡±â] LIDOCAINE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:glucose-regulated protein Drug:lidocaine Toxicity:intestinal disorder. [¹Ù·Î°¡±â] Replated Protein:Alkaline phosphatase Drug:lidocaine Toxicity:lidocaine induced hepatitis. [¹Ù·Î°¡±â] Replated Protein:C-reactive protein Drug:lidocaine Toxicity:fever. [¹Ù·Î°¡±â] Replated Protein:C-reactive protein Drug:lidocaine Toxicity:lidocaine induced hepatitis. [¹Ù·Î°¡±â] Replated Protein:Alpha-1-acid glycoprotein Drug:lidocaine Toxicity:lidocaine tolerance. [¹Ù·Î°¡±â] Replated Protein:Gamma-glutamyltranspeptidase Drug:lidocaine Toxicity:fever. [¹Ù·Î°¡±â] Replated Protein:Alkaline phosphatase Drug:lidocaine Toxicity:fever. [¹Ù·Î°¡±â] Replated Protein:Gamma-glutamyltranspeptidase Drug:lidocaine Toxicity:lidocaine induced hepatitis. [¹Ù·Î°¡±â]
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