Local Anesthetics, General Anesthetics, Opoids And Nsaids

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Local Anesthetics

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Substances that produce temporary blockade of the neural transmission when applied to nerve axons

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• Novocaine

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First injectable ester LA which metabolized in the plasma by Pseudocholisterase and is excreted by the kidneys

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• Tetracaine

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Topical ester LA that has a slow onset, long duration due to its high pKa.

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• 2-Chloroprocaine

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Ester LA with a duration of 45-60 min and rapid termination of effect. It os delivered by IV and may cause thrombophlebitis.

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• Benzocaine

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An ester LA that was the first to be developed synthetically. It is a benzoic acid derivative, is only effective in high concentrations and used mostly in the mucus membranes. May cause methemoglobinemia (disorder characterized by the presence of a higher than normal level of methemoglobin (metHb) in the blood). commonly used as a topical pain reliever

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• Lidocaine

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First amide LA that is metabolized in liver and excreted by kidneys. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery.

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• Dibucaine

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Topical amide LA with a high potency and toxicity. It is an inhibitor of plasma cholinesterase and used as a test for sensitivity to succinycholine.

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• Mepivacaine

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Similar to lidocaine but causes less vasodilation, it has slightly greater potency and duration. It is used for epidural, spinal, peripheral nerve block and local infiltration. Due to its potential for accumulation, it is unsuitable for a prolonged epidural infusion

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Bupivacaine

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Amide LA with a slow onset, long duration and has significant frequency-dependent block. Is good for spinal anesthesia as isobaric or hyperbaric solution. Adding epinephrine will add to the duration. Has a major cardiac toxicity associated with high systemic blood levels.

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Ropivacaine

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An amide LA that is pure S isomer, it is less potent and lasting compared to Bupivacaine but less cardiotoxic. It is a better frequency dependent block.

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• Prilocaine

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the most rapidly metabolized amide LA with a Ortho-Toulidine ring which produces methemoglobinemia.

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o Adjuvants(assistants) for LA

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epinephrine which may decrease absorption and prolong duration and bicarbonate which increases pH of solution and accelerate onset and decrease duration

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General Anesthetics

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compounds that have the ability to depress the CNS

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• Aspirin

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Prototype NSAID which is used an analgesic, anti-inflammatory, antipyretic, and prevents clotting. Adverse reactions include Reye’s Syndrome in infants and children, gastritis, and bleeding

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• Ibuprofen

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An analgesic or antipyretic NSAID. It is consider a weak aspirin and has a low risk for ulcers or gastritis.

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• Indomethacin

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An anti-inflammatory NSAID with a high risk for gastritis or ulcers. It is not designed for chronic use and is a good treatment for gout.

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• Ketorlac

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An analgesic and only NSAID to be delivered IV/IM.

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• Naproxen

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An anti-inflammatory NSAID with a low risk for ulcers or gastritis.

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• Piroxilam

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An anti-inflammatory NSAID similar to Naproxen. It has longer duration compared to Naproxen.

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• Acetaminophen

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An analgesic and antipyretic non-NSAID

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• Omeprazole

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a proton pump inhibitor (PPI) where it works in the stomach to lower acid production and stops irritation in stomach. Helps combat NSAID induced ulcers and gastritis.

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• Misoprostol

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A synthetic prostaglandin which increases mucus production and lowers acid production in stomach. Helps combat NSAID induced ulcers and gastritis. Can cause diarrhea

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Opioid Analgesics

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mainly centrally acting (brain and spinal cord) which are
used for severe pain.

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• Morphine

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prototype opiod analgesic that activates mu opioid receptors at multiple points along the pain pathway (including brain and spinal cord) resulting in a reduction in pain perception

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• Alfentinil

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a potent but short-acting synthetic opioid analgesic, used for anaesthesia during surgery (administered by injection for fast onset of effects and precise control of dosage. Produces strong respiratory depression.

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• Heroin

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Due to its nonpolar nature, heroin rapidly enters the brain where it is rapidly metabolized to morphine (Thus, heroin is a prodrug). Due to its rapid brain penetration, heroin causes intense euphoria. Not used clinically in the US.

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• Methadone

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an orally active long acting mu opioid receptor agonist. Methadone exhibits cross tolerance with morphine or heroin and therefore is useful as a treatment for heroin addicts.

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• Meperidine

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a weak mu opioid agonist that is widely used for analgesia during delivery. It does not delay the birth process and does not antagonize oxytocin. CAUTION: use of meperidine with MAO inhibitors causes severe reactions (respiratory depression, excitation, delirium and convulsions). It is delivered as a powder, IV, or PO. Has a duration for 6 hours but can lead to addiction and respiratory depression.

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• Codeine

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a natural compound found in the poppy plant. It is weak mu opioid agonist used as an antitussive and as an analgesic in mild pain. Codeine is considered a prodrug, since it is metabolized in vivo to the primary active compounds morphine and codeine-6-glucuronide. Codeine is also combined with NSAIDs.

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• Oxycodone

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a weak opioid agonist used in combination with NSAIDs for analgesia (oxycodone plus aspirin = PERCODAN; oxycodone plus acetaminophen = PERCOCET).

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• Fentanyl

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a short acting, but powerful opioid analgesic used for coming out of surgery with a potency approximately 100 times that of morphine. Used for breakthrough pain. It is also available as a transdermal patch (DUROGESIC/DURAGESIC) for continuous delivery. It is the most highly abused narcotic drug that has a duration for 10-15 minutes. Overdose can cause respiratory depression.

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• Remifentanil

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a potent ultra short-acting synthetic opioid analgesic given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is used for sedation as well as combined with other medications for use in general anesthesia. The use of remifentanil has made possible the use of high dose opioid and low dose hypnotic anesthesia, due to synergism between remifentanil and various hypnotic drugs and volatile anesthetics.

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• Propoxyphene

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a mu opioid agonist that is used for mild to moderate pain. It is commonly given in combination with aspirin or acetaminophen FDA warning “Propoxyphene in high doses, taken by itself or in combination with other drugs, has been associated with drug-related deaths. Do not take propoxyphene in combination with other drugs that cause drowsiness: alcohol, tranquilizers, sleep aids, antidepressant drugs, or antihistamines.

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• Sufentanil

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a powerful synthetic opioid analgesic, approximately 5 to 10 times more potent than its analog, fentanyl used during surgery. It is a potent ultra short-acting synthetic opioid analgesic given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Sufentanil causes significant respiratory depression and may cause respiratory arrest if given too rapidly

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• Loperamide

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a mu opioid agonist that is poorly absorbed after oral administration. Since it is retained in the GI tract it has low abuse potential and is used as an antidiarrheal. Loperamide does not cross the blood-brain barrier in significant amounts, and thus it has no analgesic properties. Any loperamide that does cross the blood-brain barrier is rapidly exported from the brain by P-glycoprotein. Tolerance in response to long-term use has not been reported.

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• Buprenorphine

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Buprenorphine is a partial agonist at μ-opioid receptors but a κ-opioid receptor antagonist. Intravenous bupernorphine before induction of anesthesia is more effective and has fewer side effects than morphine in post operative pain management. Can act on kappa receptors as well.

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• Tramadol

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This orally acting analgesic weakly binds to opioid receptors and inhibits the uptake of NE and serotonin. Tramadol is used for mild to moderate pain.

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• Nalbuphine

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produces a lower incidence of post operative nausea and vomiting compared to morphine and is used to supplement anesthesia during surgery. Nalbuphine is also indicated for use during labor. It is noteworthy in part for the fact that at low dosages, it is found to be much more effective analgesic by women than by men, and may even increase pain in men

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• Butorphanol

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a mixed agonist-antagonist with low intrinsic activity at μ-opioid receptors but an agonist at k-opioid receptors.

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• Pentazocine

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kappa opioid receptor agonist and a mu opioid receptor antagonist. Pentazocine is more likely to cause hallucinations and other psychotomimetic effects; cardiovascular effects make it unsuitable for use in myocardial infarction. Unlike morphine its respiratory depressant action is subject to a "ceiling" effect. It can be used as an analgesic for dental extractions except in heroin addict patients.

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Nitrous oxide

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Inert gas that is used as an fast inducer. has no metabolism and overdose can cause anoxia

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Isoflurane

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A gas with a fluorine in its structure. It is metabolized in the liver where the fluorine is released. It is a complete anesthetic and most commonly used in OR. Overdose can cause kidney damage due to long time fluoride exposure

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Propofol

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A liquid by IV drip that has no metabolism and good for 4 hours. It is a quick inducer and is a complete anesthetic. Overdose will lead to anoxia, respiratory distress and death.

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Thiopental

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Also known as truth serum, could be delivered by IV or patch and has a duration for 30-60mins. It is a fast inducer used in surgery but Overdose can cause Respiratory depression.

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Midazolam

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Can be delivered by tablet (PO) or by IV. Has a duration for 2-4 hours and is a partial anesthetic which is good for for short surgical procedures. Overdose can cause respiratory depression.

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Flumazemil

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An antidote for meperidine that is given by IV. Has a duration for 2-6 hours.