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    LECTURE 3 - Pharmacology of Vasoconstrictors

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    KIH 20162017
    This document discusses vasoconstrictors used with local anesthetics. It explains that local anesthetics alone are vasodilators, increasing absorption and decreasing duration of anesthesia. Vasoconstrictors like epinephrine counteract vasodilation by constricting blood vessels, slowing absorption and prolonging anesthesia. Epinephrine is preferred over norepinephrine due to fewer side effects. Levonordefrin is also used as a vasoconstrictor. Selection depends on the procedure and patient's medical status. Contraindications include uncontrolled hypertension and severe cardiovascular disease.

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    LECTURE 3 - Pharmacology of Vasoconstrictors

    Uploaded by

    KIH 20162017
    280 views27 pages
    This document discusses vasoconstrictors used with local anesthetics. It explains that local anesthetics alone are vasodilators, increasing absorption and decreasing duration of anesthesia. Vasoconstrictors like epinephrine counteract vasodilation by constricting blood vessels, slowing absorption and prolonging anesthesia. Epinephrine is preferred over norepinephrine due to fewer side effects. Levonordefrin is also used as a vasoconstrictor. Selection depends on the procedure and patient's medical status. Contraindications include uncontrolled hypertension and severe cardiovascular disease.

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    This document discusses vasoconstrictors used with local anesthetics. It explains that local anesthetics alone are vasodilators, increasing absorption and decreasing duration of anesthesia. Vasoconstrictors like epinephrine counteract vasodilation by constricting blood vessels, slowing absorption and prolonging anesthesia. Epinephrine is preferred over norepinephrine due to fewer side effects. Levonordefrin is also used as a vasoconstrictor. Selection depends on the procedure and patient's medical status. Contraindications include uncontrolled hypertension and severe cardiovascular disease.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    280 views27 pages

    LECTURE 3 - Pharmacology of Vasoconstrictors

    Uploaded by

    KIH 20162017
    This document discusses vasoconstrictors used with local anesthetics. It explains that local anesthetics alone are vasodilators, increasing absorption and decreasing duration of anesthesia. Vasoconstrictors like epinephrine counteract vasodilation by constricting blood vessels, slowing absorption and prolonging anesthesia. Epinephrine is preferred over norepinephrine due to fewer side effects. Levonordefrin is also used as a vasoconstrictor. Selection depends on the procedure and patient's medical status. Contraindications include uncontrolled hypertension and severe cardiovascular disease.

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    Pharmacology of

    Vasoconstrictors
    Semua anestetik local vasodilator: Procain paling
    kuat. Prilocain dan mepicaine paling lemah.
    Setelah injeksi anestetik local akan terjadi dilatasi
    pembuluh darah
    1. An increased rate of absorption of the local
    anesthetic into the cardiovascular system, which in
    turn removes it from the injection site
    (redistribution)
    2 Higher plasma levels of the local anesthetic, with
    an attendant increase in the risk of local anesthetic
    toxicity (overdose)
    3 Decrease in both the depth and duration of
    anesthesia because the local anesthetic diffuses away
    from the injection site more rapidly
    4 Increased bleeding at the site of treatment
    What happens if you dont use a vasoconstrictor?
    *Plain local anesthetics are vasodilators by nature

    1) Blood vessels in the area dilate


    2) Increase absorption of the local anesthetic into the
    cardiovascular system (redistribution)
    3) Higher plasma levels increased risk of toxicity
    4) Decreased depth and duration of anesthesia diffusion
    from site
    5) Increased bleeding due to increased blood perfusion to the
    area
    1) Patient is not numb as long without
    epinephrine

    2) Patient is simply not as numb

    3) More anesthetic goes into the circulation

    4) Increased bleeding; more blood to area


    Vasoconstrictors
    Adrenergic drugs and are called
    sympathomimetic, or adrenergic drugs

    1) Constrict blood vessels decrease blood flow to the surgical site

    2) Cardiovascular absorption is slowed lower anesthetic blood levels

    3) Local anesthetic blood levels are lowered lower risk of toxicity

    4) Local anesthetic remains around the nerve for longer periods


    increased duration of anesthesia

    5) Decreases bleeding
    Chemical Structure
    Classification of Adrenergic Drugs
    Classification by chemical structure is related to the
    presence or absence of a catechol nucleus
    Catechol is orthodihydroxybenezene
    Sympathomimetic drugs that have a hydroxy (OH-)
    substitution in the 3rd and 4th positions of the aromatic ring
    are termed catechols
    Catecholamines
    If the 3rd and 4th positions contain an amine group (NH2) attached to
    the aliphatic side chain, they are then called catecholamines

    Epinephrine
    Norepinephrine natural catecholamines of sympathetic NS
    Dopamine

    Isoproterenol
    and synthetic catecholamine
    Levonordefrin
    Chemical Structure
    Catecholamines Noncatecholamines
    *Epinephrine Amphetamine
    *Norepinephrine Methamphetamine
    *Levonordefrin Ephedrine
    Isoproterenol Mephentermine
    Dopamine Hydroxyamphetamine
    Metaraminol
    Methoxamine
    Phenylephrine
    Modes of Action
    3 Classes of Sympathomimetic Amines:
    1)*Direct Acting directly on adrenergic receptors
    2) Indirect Acting use norepinephrine release
    3) Mixed Acting both direct and indirect actions
    2 Types of Adrenergic Receptors:
    1) Alpha
    -contraction of smooth muscle in blood vessels
    -vasoconstriction
    -Alpha 1 excitatory; post-synaptic
    -Alpha 2 inhibitory; post-synaptic

    2) Beta
    -smooth muscle relaxation
    -vasodilation/bronchodilation
    -cardiac stimulation, i.e., increased
    rate and strength of contraction
    2 Types of Beta Receptors:

    1) Beta 1
    -found in heart and small intestines
    -produces cardiac stimulation and lipolysis

    2) Beta 2
    -found in bronchi of the lung, vascular beds
    and uterus
    -produces bronchodilation and vasodilation
    The dilution of vasoconstrictors is commonly referred to as a
    ratio i.e., 1:50,000; 1:100,000; 1:200,000 etc,

    A concentration of 1:1,000 means that there is 1 gram


    (1000 mg) of solute (drug) contained in 1000 ml (1 L) of
    solution, therefore, 1:1,000 dilution contains 1000 mg
    in 1000 ml or 1.0 mg/ml of solution (1000 ug/ml)

    The concentration of 1:1,000 is very concentrated


    (strong); a much more dilute form is used in dentistry
    for example, 1:50,000 > 1:100,000 > 1:200,000
    (1:100,000 = 0.01 mg/1 ml of solution)
    Norepinephrine
    NOREPINEPHRINE
    Norepinephrine lacks Beta 2 actions (bronchodilation and
    vasodilation) and produces intense peripheral vasoconstriction
    with possible dramatic elevations in blood pressure

    Norepinephrines side effect ratio is 9 times higher than


    epinephrine

    Norepinephrines use in dentistry is not recommended and its


    use is diminishing around the world

    Epinephrine remains the vasopressor of choice in dentistry

    *Norepinephrine is not used because of its many side effects


    Epinephrine
    Epinephrine
    Sodium Bisulfite antioxidant added
    18 months shelf life
    Acts directly on Alpha and Beta receptors
    Beta effects predominate
    Increases force / rate of contraction
    Increases stroke volume
    Increases myocardial O2 use
    Increases cardiac output / heart rate
    Increases dysrhythmias and PVCs
    Increases coronary artery perfusion
    Increases systolic blood pressure
    Decrease in cardiac efficiency
    Alpha receptor stimulation leads to hemostasis initially

    Beta 2 actions predominate leading to vasodilation 6 hours after


    a surgical procedure

    Potent bronchodilator (asthma)

    Not a potent CNS stimulant

    Increases oxygen consumption in all tissues of the body

    Reuptake by adrenergic nerves terminates epinephrine action

    Ventricular fibrillation is possible


    Clinical Applications of Epinephrine
    1) Management of acute allergic reactions
    2) Management of bronchospasm
    3) Management of cardiac arrest
    4) Vasoconstrictor for hemostasis
    5) Vasoconstrictor to decrease absorption into CVS
    6) Vasoconstrictor to increase depth of anesthesia
    7) Vasoconstrictor to increase duration of anesthesia
    8) To produce mydriasis (excessive pupil dilation)
    Levonordefrin
    Levonordefrin is freely soluble in dilute acid
    solutions

    Sodium bisulfite is added to delay its deterioration

    Synthetic vasoconstrictor

    Acts through direct Alpha receptor stimulation


    (75%)

    Acts through some Beta activity (25%)


    Levonordefrin produces less cardiac and CNS stimulation
    than epinephrine

    Levonordefrin is eliminated via COMT (catechol-O-methyl


    transferase) and MAO (monamine oxidase)

    Levonordefrin is obtained via Mepivacaine 1:20,000; used at


    a higher concentration, i.e., 1:20,000 because it is
    1/6th as potent as epinephrine

    Levonordefrin has a maximum recommended dose of 11


    cartridges
    -Levonordefrin is only 1/6th as strong as
    Epinephrine, therefore, using a ratio of
    1:20,000 Levonordefrin is like using a ratio of
    1:120,000 of Epinephrine

    -you will need more Levonordefrin because it is


    only 15% as effective as Epinephrine
    Selection of a vasoconstrictor depends on:
    1) Length of the dental procedure
    2) Requirement for hemostasis
    3) Requirement for post-operative pain control
    4) Medical status of the patient
    Contraindications to Using Vasoconstrictors
    1) Blood pressure > 200/115 mm Hg

    2) Severe cardiovascular disease ASA IV+

    3) Acute myocardial infarction in the last 6 months

    4) Anginal episodes at rest

    5) Cardiac dysrhythmias that are refractory to drug treatment

    6) Patient is in a hyperthyroid state of observable distress

    7) Levonordefrin and Norepinephrine are absolutely


    contraindicated in patients taking tricyclic antidepressants
    (Elavil, Sinequan)
    References
    Malamed, Stanley: Handbook of Local Anesthesia. 5th Edition. Mosby. 2004

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