(Aspirin)

Acetylates COX (1&2) enzymes,irreversible inhibition;

Inhibits platelet aggregation;

Tx inflammation, fever, pain, HA, arthritis, dysmenorrhea, RA (large dose);

SE - GI ulcer, tinnitus, hearing loss, hepatic injufy, Reyes', asthma, ↑ bleeding time; CI with bleeding disorders

(Tylenol)

NSAID

Inhibitor of COX-1,2,(3);

analgesic and antipyretic;

NOT useful for anti-inflammatory;

SE - HEPATOTOXICITY; No effects on platelets, NO GI IRRITATION

NSAID - POTENT;

anti-inflammatory, analgesic, antipyretic;

Tx gout, arthritis; Used to close Ductus Arteriosus;

SE - GI IRRITATION, CNS effects (HA, dizziness, depression), renal dysfxn;

CI in pregnancy*

(Advil, Motrin)

NSAID

Reversible COX inhibitor; Alters platelet (prolonged bleeding),

anti-inflammatory, antipyretic, analgesic;

Tx RA (3200mg), pain (400mg/6hrs);

SE- GI irritation (less than others);

CI in pregnancies*

(Aleve)

NSAID

Reversible COX inhibitor; Alters platelet (prolonged bleeding),

Anti-inflamm, antipyretic, analgesic;

Long half-life - 14hrs, so 2xday dosing;

SE- GI irritation

NSAID - reversible COX inhibitor;

Alter platelet (prolonged bleeding),

anti-inflamm, antipyretic, analgesic;

LONG HALF-LIFE - 40hrs, once a day;

SE- GI irritation

NSAID - heteroaryl acetic acid deriv;

POTENT analgesic, SHORT-TERM USE ONLY;

moderate anti-inflammation effects;

IM, oral, parenteral admin;

Tx post-op pain and inflamm, topical for eye inflammation (allergies or post-op);

NSAID - heteroaryl acetic acid derivative;

Potent COX inhibition;

Tx RA, OA;

SE - GI, elevation of hepatic aminotransferase activity;

CI for pregnancy

Diclofenac + Misoprostol

NSAID + PGE1 agonist - heteroaryl acetic acid derivitive; gastric protection

PGE1 analog;

gastric protection

Given with GI upsetting drugs

NSAID - Enolic Acid;

Anti-inflamm, antipyretic, analgesic;

Equiv w/ asprin, indo, naproxen;

LONG HALF-LIFE - 50hrs, one a day;

SE - GI, RENAL (high risk);

Drug interaction - lithium (reduce clearance)

NSAID - Enolic Acid;

More selective for COX2 (but still blocks 1);

LONG HALF-LIFE - one a day;

Tx OA, RA;

SE - GI (better than others)

(Celebrex)

NSAID - selective COX2;

Anti-inflamm, antipyretic, analgesic;

Tx OA, RA, acute pain, dysmenorrhea;

SE - CV*, some GI uleration, dyspepsia, inhibits labor, renal alteration, hypersensitivity rxns;

Drug interaction- "heart meds", diuretics, coumadin

MuOR Agonist (minimal kappa action);

Active itself but converted to M-6-glucaronide = 100x potency;

4 hr half life - accumulation;

extensive (70%) first pass metabolism (doses when given PO must be much higher than when IV); given PO/IV/PR

Tx: mod/severe pain;

Use in pts taking MAO-Is;

SE - tolerance, constipation, renal clearance* (potential toxicity in renal failure pt)

MuOR agonist (morphine-like);

PO and/or parenteral admin;

Tx mod/SEVERE pain

SE: constapation, repsiratory depression

*Good option for pt with renal insufficency (no active metabolites to accumulate)

MuOR agonist (morphine-like);

long acting;

Tx mod/severe pain;

High abuse potential*

SE: Opiate SE

(Demerol)

MuOR agonist (morphine-like);

50% inactivated, first pass (medium Oral:IV potency);

Tx mod/severe pain;

less spasmogenic, no miosis, less constipation;

SE: Toxic met. (normeperidine) can accumulate to produce seizure risk (esp in Renal Failure); Anticholinergic effects* peripherally causes dilation of the pupils, constipation, tachycardia and centrally causes agitation, confusion, hallucination)

CI - lethal w/ MAO-inhibitors, CHILDREN

In summary: Exception to the triad of opiate abuse (casues tachycardia and pupil dilation, not pinpoint), not a very good analgesic, lots of SE (there are better choices out there)

MuOR agonist (morphine-like);

PO admin; single daily dose;

Long half life (8 to 120 hours depending on pt);

Tx - abuse withdrawl/cravings, (> 180 mg/d is withdrawl, less is maintaince) dampen peaks/troughs of drug concentrations during weaning

 Pt may have to remain on Methadone for life.

SE: CYP and aromatase inhibition (↓ testosterone/libido: ED), prologation of QT (trousades, arrhythmia)

Drug of choice in Pregnancy**

Dose escalation may be req towards the end of pregnancy.

MuOR agonist (morphine-like);

Transdermal patch for chronic admin, IV for anesthesia;

Low Oral:IV potentcy

Tx: mod/severe pain (80x potency); 

Use in pts taking MAO-Is;

Opiate SE

 Warn pt with fever! High temps increase drug delivery from transdermal patches, may cause inadvertant OD.

Potentially lethal toxicity when patch is consumed in other ways (chewing, PR etc...)

*Good option for pt with renal insufficency (no active metabolites to accumulate)

MuOR agonist (morphine-like);

anesthesia IV; rapid onset, short duration

Tx: mod/severe pain

Opiate SE

MuOR agonist (morphine-like); Low affinity, 10% conv to morphine (morphine in tox screen of pt on codeine);

PO or parenteral admin; renal clearance,

Resistance in 10% caucasians;

Tx: mild pain, cough suppressant (action @brainstem cough pattern generator, rapid development of tolorance, some debate as to its efficacy as an anti-tussive agent)

Opiate SE + Accumulates in pt with Renal Failure + potential for toxicity in ultrarapid CYP2D6 metabolizing breast feeding mothers

MOR agonist (morphine-like);

long duration of action (8-12 hrs);

Tx: severe pain

Opiate SE

MuOR partial agonist/mixed agonist/antag (low action), KOR antagonist (dec abuse potential); 

PO, SL admin;

Tx: addiction/abuse;

 Potential to come off of this drug eventually.

SE - abstinence syndrome (aka withdrawl if morph-dependent), can be abused IV.

Often combined with Naloxone in SL tablets to reduce potential for abuse (if injected, naloxone precipitates withdrawl)

Opioid mixed agonist/antagonist (partial agonist);

Binds and inactivates MOR; activates KOR;

Tx: mod/severe pain, but analgesic effect is sl. dec;

Nno constipation, no respiratory depression*;

SE - abstinence syndrome;

Opioid mixed agonist/antagonist;

bind and inactivates MOR; activates KOR;

Tx mod/severe pain, but analgesic effect is sl. dec;

no constipation, no respiratory depression;

SE - abstinence syndrome;

Opioid receptor antagonist;

LONG DURATION (hrs if PO, days if IM);

PO, IM admin (not a good choice for emergency opiate OD, not avail IV*),

↓ alcohol cravings by ↑ baseline release of β-endorphins

Tx: Used in addiction maintinance programs (cangive single doses on alternate days), alcohol abuse/addiction

Opioid receptor antagonist;

Long duration of action (11 hr);

IV, SC, IM

Tx: opioid OD

* Better choice than Naloxone (t_1/2 shorter than morphine) or Naltrexone (not avail IV).

Opioid receptor antagonist;

IV only: rapid onset, short duration (esp compared to morhphine), dose accordingly;

EXTENSIVE P.O. FIRST PASS METABOLISM;

Tx: opioid OD, reverses respiratory depression;

Can cause opioid withdrawal; start low, go slow (titrate up dose), can also wear off before opiates do causing the pt to relapse into respiratory depression.

NMDA receptor blocker, SSRI (+multiple other effects)

opiate derivative; no analgesia; acts on non-opioid receptors;

Tx: prevention of surgery-induced sensitization, neuropathic pain, cough suppression (found in many OTC cough meds: Robbatussin, dymatapp, delsym...);

SE: Dizziness, confusion, fatigue, hallucinations

Habit-forming*

(Imodium)

Opiate derivative;

dec GI motility, peristalsis and secretion = inc absorption;

Tx diarrhea;

no CNS effects - doesn't cross BBB (no analgesia/euphoria/addiction potential)

OP-3

Endorphins naturally bind well

analgesia; dec respiration; dec GI activity

OP-1

Enkephalins naturally bind well

analesia; GI regulation; autonomics

OP-2

Dynorphins naturally bind well

analgesia; hallucinations

Sedatives/hypnotics (↑ CNS depression incl respiratory depression);

Antipsychotic tranquilzers (↑ sedation, CV effects)

Sympathomimetics;

Antihistamines;

MAO inhibitor antidepressants (rel CI to all opiates, high incidence of hyperpyrexic coma)

Na+ channel blocking anti-epilleptic

Adjuvant for analgesia/opioids;

Tx: neuropathic pain (damage or infiltrate)

Benzodiazepine

Adjuvant for analgesia/opioids;

Tx neuropathic pain (damage or infiltrate)

Adjuvant for analgesia/opioids;

TCA

Tx neuropathic pain (damage or infiltrate)

Centrally and presynaptically-acting α2 agonist (dec Ca2+ influx and thereby dec vessicle release of NT)

Used as an adjuvant for analgesia/opioids; enhances opioid analgesia

Tx: opiate addiction in an outpatient setting (effective tx of craving, piloerection, anxiety and agitation)

SE: Dry mouth, sedation, constipation

 Enkephalin (OP-1, delta)

Dynorphin (OP-2, kappa)

β-endorphin (OP-3, mu)

"Special K" - street drug related to angel dust

NMDA receptor blocker

Tx: Used preemptively to prevent surgery-induced sensitization, neuropathic/severe pain, cough suppression

SE: Hallucinations, amnesia, CV pressor effects (cause ↑ ICP)

Na+ Channel Blocker (blocks transmission of pain signals along neurons)

Tx: Trigeminal Neuralgia and as an anti-convulsant

Behavioral restlessness (dysphoria), Somnolescence/Mental clouding, Sedation, Respiratory Depression, Antidiuresis, Nausea/Vomiting, Iching aroudn the nose, postural HypoT.

Bradycardia

Miosis, Convulsions (inc ICP), Constapation

Weak MuOR agonist

Metabolized to Morphine (strong MuOR) and 6-MAM

Undergoes extensive first pass metabolism to morphine, IV admin eliminates this (bigger high).

Highly addictive

SE - dependance/addiction, constapation

Due to metabolism, high levels of morphine (not heroin itself) will be found in the urine tox screen (EIA) of a person on heroin (>15,000 ng/ml) with high Morpine:Codine ratios (>2:1, normally much greater, indicates heroin or poppyseed over morphine alone)

What can be detected by EIAs?

What cannot?

EIA: Enzymatic Immunoassays (Ab-based test used in standard urine tox screens)

Detects: Morphine, Heroin (6-MAM), Hydrocodone and Codine

*Heroin and Codine identified based on ratio of Morphine:Codeine based on their metabolism (>2:1 = heroin, <2:1 =Codiene)

Cannot detect synthetic/semisynthetic opiates: Oxycodone and hydromophone

Poppy seeds

Fluroquinilone Abx*

Binds the α-2-δ subunit of V-gated Ca2+ channels causing them to be internalized.

Can reduce the hypersensitization effects of Ca2+ channel upregulation that can occur in central pain sensitization.

PO admin, renal excretion

Tx: pain (ancillary, w/opiates, particularily useful for neurogenic and/or post-stroke pain)

Ancillary drug for pain

Blocks V-gated Na+ channels decreasing the propogation of pain signals. Blockades synaptic transmission in trigeminal nucleus.

Tx: Neuropathy, stroke, MS, phantom limb syndrome, trigeminal neuralgia.

SE: BLACK BOX: Steven-Johnson Syndrome (potentially fatal epidermal necrolysis)

Diplopia, dizziness, drowsiness.

Suicidal Ideation*

Induces its own CYP metabolism!

Watch in liver failure pt. Also, dose escalation is often required.

Ancillary drug for tx pain (used w/ opiates); useful as chronic pain is often associated with major depression;

Inhibits NE and 5-HT reuptake

SE: CYP2D6 interactions (watch with Codiene), dizziness, HA, drwosiness, memory impairment.

Drugs ending in "-ine": Amytryptyline, Nortriptyline, Ipramine, Dispiramine

Adjuvant for analgesia/opioids;

TCA

Tx neuropathic pain (damage or infiltrate)

Adjuvant for analgesia/opioids;

TCA

Tx neuropathic pain (damage or infiltrate)

Rx Opiate agonist

Tx: Diarrhea

No analgesia at recommended dose but high doses have CNS effects and addiction potential.

Commercial preparations contain atropine to discourage this.

Oxycodone + Acetaminophen

New limits on how much acetaminophen can be included (severe liver damage potential)

Hydrocodone + Acetaminophen

Acetaminophen component has recently been limited due to its potential to cause severe liver damage.

Contain Mg2+

Mg is a key regulator of the NMDA receptor which mediates pain signals.

Other Herbal Pain Remedies

Capsacin (topical pain relief), Cod-liver oil (systemic musculoskeletal pain relief), Devil's Claw (oral, arthritic pain) and White Willow (Oral, for low-back pain)

MuOR agonist

Tx: Pain

Opiate SE

MuOR agonist

Tx: Pain

Opiate SE

MuOR Agonist

Tx: pain

Opiate SE

MuOR Agonist

Tx: Pain

Opiate SE