Pharmacology

• has a sensory and emotional component, very hard to explain to a person who hasnt felt it before and its a complex, and subjective experience.
• overall pain is undertreated! common reason for a doctors visit. Many will ignore many things but when they are in pain it FORCES them to come in.

pain perception by CNS, involves tissue damage, radiating pain can be felt, you can feel the pain, this is a normal signal process. Nervous system is working normally and activated

where the pain starts. it is the process of converting the "stimulus" (smashed finger, burned finger) into a pain impulse.

NSAIDS, Local Anesthetic work

nerve impulses generated by stimulus travel up the spinal cord and are transmitted to the brain via NT

Opioids, GABA analogs (baclofen) (gabapentin)

from the brain the impulses stimulate another area such as: thalamus, contralateral (opposite side) somatosensory cortex and limbic system

information is perceived or interpreted by location, intensity and quality

General Anesthetics

attenuate pain or "lessen" it, by inhibitory input from brain (endorphins, NE, GABA)

Opioids, SSRI's, TCA's, gabapentin

Nervous System/sensing is damaged and is NOT functioning normally. central or peripheral. Burning, tingling, shooting, numbness. Ex. diabetes neuopathy, shingles started with an infection even after it heals the pain can still be there.

due to tissue trauma, will go away when situation resolves. Labor, cut

• Old Definition: 3-6 months beyond onset
• New Definition: pain that serves no adaptive purpose and disrupts sleep and normal living

can be nociceptive or neuropathic or BOTH

Pain related to cancer, we can determine cause of why in pain

persistent pain that is not associated with cancer, pain itself is considered the disease. The pain consumes the patient. There is no apparent cause

body adapts to a drugs effects which results in needing more drug, Exposure of the drug results in changes or a lessening of one of the drugs affects. Can build up a tolerance of the drugs side effects or to the drug itself. = we need more.

when you take a drug away they have a withdrawl sx

addictive behaviors, compulsive use, craving, breaking law to get drug, pyschological, out of control

pain, its a self/subjective report, personalized. Go with what the patient SAYS

• used for acute: mild-moderate pain
• APAP, NSAIDs,
• non-selective: ibuprofen (Motrin)
• selective cox 2 Celeboxib (Celebrex)

APAP, Tylenol

• Usually used in combination with things:
• Ex. Tylenol PM has benedryl w/ it
• Tylenol #3 has codeine with it.
• Lortab & Davocet N 100 has an opioid with it
• Ultracet=APAP + tramadol

• centrally acting (analgesic) or pain reliever
• blocks pain by inhibiting prostaglandin synthesis in CNS
• lowers fever by hypothalamus (antipyretic effect)

• usually takes 30 minutes-1hr
• NO ANTI INFLAMMATORY EFFECTS

• 2-500mg q 8 hrs = 4g total, maximum (limit)
• ingesting 10-15 grams results in severe hepatotoxicity (liver)
• if your a EtOH drinker or have liver problems you max intake of APAP per day is <2 g in 24 hour period

blocks the enzyme cyclooxygenase (COX) which inhibits prostaglandin synthesis and has anti platelet effects by blocking thyroxane

• anti-pyretic effects
• anti-inflammatory effects

S/E: GI ulcer, prolonged bleeding

MIDDLE GUY: drug of choice for doctors who have pts where Ibuprofen and tylenol not enough but they dont want to rx Lortab or Vicodin

moderate pain, works by a "dual" or two ways to help with pain. Weakly binds to (mu) opiod receptors AND inhibits uptake of NE and serotonin

S/E: GI upset, drowsiness, enhance seizures by (lowering seizure threshold), diaphoresis

withdrawl. Can also get this affect if you give an antagonist cuz it "plugs" up all the receptors that you were using when you were orinally taking the drug for.

• has tylenol in it
• Ultracet, Darvocet

• Opioids. 1.Analgesia-pain relief, 2. Antitussive-cough suppressant, 3. Antidiarrheal-slows gut motility
• Derived from: Poppyplant, Morphine was 1st prototype

Opiates: morphine like, "naturally" derived,

Narcotic drugs/Narcotics: (slang) morphine like with both analgesic and sedative properties. Carries a connotation of bad or negative! Lunesta commercials specifically state this is a NON NARCOTIC drug. Makes it okay to take.

OPIOID: refers to the morphine like drug and refers to both natural AND synthetic compounds

binds at opiod receptors in CNS and GI tract. Once bound the "transmission" is inhibited or stopped from the periphery to the spinal cord by activation of the inhibitory or modulation pathway such as GABA, NE which slows down or inactivates that nerve impulse. So we get a relief from the somatic sensation of pain. or feeling of... physical pain. Also alterations of the limbic system occur=happy, feel good, euphoria

• 1. (Mu) opioid receptor: this is the one we are really targeting when we want to get people out of pain! S/E: inhibit slow RR and inhibit slow GI
• 2. Delta:
• 3. Kappa:

Opioids for analgesia (pain)

antitussive effect attained with a lower dose then required for the analgesic effect. Not need as much if your just trying to slow down the cough it will NOT completely STOP it.

• Robutussin Dextromethorphan (DM)-OTC. lack of analgesic effects, less addictive and doesnt cause as much constipation.
• Usually combined with guaifenesin which "liquifies" the mucous to it comes/coughs up easier. Hopefully every cough you do have should be a productive cough.
• Dont use OPIOIDS in kids<6 (cough syrups)
• Codeine: S/E constipation
• hydrocodone: S/E constipation

specific GI effects. reduce peristaltic effects, increase water absorption and alleviate diarrhea. Dont have CNS affects. These special opioids target the GI receptors

• Immodium AD: Loperamide, OTC
• Lomotil: Diphenoxylate, RX

• 1. CNS: analgesia, euphoria, sedation, decrease RR, cough suppression, miosis, nausea, temp (raise, decrease)
• 2. Cardiovascular: bradycardia, hypotension, intracranial pressure
• 3. GI: decrease peristalsis, constipation,
• 4. Renal: anti-diuretic effect
• 5. GU: reduced uterine tone, prolonged/slows down labor (ex. Nubane)

pain but the S/E is slowing of uterus or uterine contractions

1. Euphoria, 2. Sedation, 3. RR decrease, 4. Miosis (constriction of pupils), 5. N&V, 6. Constipation, 7. Pruritis (itching)

A tolerance can build up to most SE but not all with continued use

pleasant, floating sensation, feels good! Does not automatically mean addiction! Tolerance will develop. Dysphoria (anxious, excited) is possible and is an idiosyncratic effect.

drowsiness, mental "clouding", caution driving ect. reaction time is slowed. CNS depressing agent. Tolerance will occur.

most feared SE of opioids. Tolerance will build up!This is what will kill individuals in an overdose. Stages occur. You go to sleep, deep sleep, do not wake up due to respiratory arrest.

Especially to a opioid naive. All 12 hours of drug will be released at the same time!!!

constriciton, pinpoint pupils. NO TOLERANCE DEVELOPS!! Mediated by parasympathetic pathways. Take opioids for long time, miosis occurs. That is just how it is. Walk around all the time. Doesnt mean they are addicted.

opioids active the brainstems chemoreceptor trigger zone (CTZ). Which=N&V. Tolerance does occur. Can be minimized by taking with food and refraining from activity. Anti-emetic drugs are added to help.

do not build up a tolerance! Long term opioid use require a bowl regimen which includes laxatives on a schedule. Such as Miralax. DO NOT use bulk forming laxatives like Metamucil. It can make it worse! Needs to be slow and controlled not just BAM WHAM!

opioids can cause a itchy skin rxn. Fentanyl appears to be the one to grab if we have a patient who easily breaks out. Tx with antihistamines or tx with switching opioids. DONT know if it build up tolerance. Some do, Some dont!

• 1. Phenanthrenes
• 2. Phenylheptylamines
• 3. Phenylpiperidines
• 4. Morphinana
• 5. Benzomorphans

• Strong: Schedule II
• Morphine
• Hydromorphone
• Oxymorphone
• Heroine (diacetylmorphine)

• Moderate: Schedule II
• Oxycodone
• Hydrocodone
• Codeine breaks or metabolizes into morphine

• Agonist/Antagonist:
• Nalbuphine
• Buprenorphine

• Strong:
• Methadone

• Weak:
• Propoxyphene

• Strong:
• Fentanyl
• Meperidine

• Weak:
• Diphenoxylate
• Loperamide

• Rectal suppositories (morphine, hydromorphone)
• Transdermal Patch (fentanyl)
• Intranasal Spray (butorphanol)
• Buccal Lozenge (fentanyl)
• Pt. controlled button: