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102 Cards in this Set
- Front
- Back
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- many receptors (Mu, kappa, delta)
- effect pain transmission Effects: - analgesic effects - sedation & mental clouding - Emesis (chemoreceptor trigger zone) - Respiratory depression (useful in pulmonary edema) - Miosis (pupil constriction) - truncal rigidity - bradycardia - Seizures - Constipation (be proactive about preventing this) - harder to urinate (worse in BPH) - prolong labor - Release of histamine that can cause flushing, itching & sweating (more common when injected) - chronic use leads to tolerance - physical dependence occurs and withdrawal when stopped abruptly (no tolerance to miosis, constipation or seizures) - give clonidine for withdrawal tx CI: - head trauma (elevated intracranial pressure) - pregnancy - impaired pulmonary function - kidney or liver problems - addison's disease |
Opiods
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- Strong opiod agonist
- stimulates all opiod receptors & produces all effects - useful in severe pain - high first pass metabolism makes it more effective Injected than oral - When injected causes itching, nausea & vomiting - can produce euphoria "floating" SE: - CNS depression in overdose CI: - head trauma (elevated intracranial pressure) - pregnancy - impaired pulmonary function - kidney or liver problems - addison's disease |
Morphine
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- Strong opiod agonist
- analgesic more potent than morphine - good to use in renal dysfunction - less likely to cause histamine release (itching) |
Hydromorphone
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- strong opiod agonist
- similar to Fentanyl but shorter half life |
Alfentanil, Sulfentanil, Remifantanil
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- Strong opiod agonist
- Schedule 1 drug - can't be legally prescribed in US - commonly abused - produces euphoria |
Heroin
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- Strong opiod agonist
- used to reduce symptoms of opiod withdrawal (given to Heroin addicts) - used in long term control of pain because effective in hard to tx types of pain |
Methadone
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- Strong opiod agonist
- effects reversed by naloxone - surgical drug (short surgical procedures w/ midazolam; & long surgical procedures because of good Cardiovascular profile) - used in lollipops & patches - high abuse potential - can cause truncal rigidity if given too fast - CYP3A4 metabolism |
Fentanyl
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- Strong Opiod agonist
- The "exception" opiod - can cause euphoria - no miosis - Doesn't suppress cough - can cause tachycardia - can cause restlessness & hyperactivity - used to decrease shivering during emergence from anesthesia SE: - cause excitement in overdose - Seizures CI: - never give with MAOI!! (serotonin syndrome) - Seizure hx - Dont use for more than 48 hours |
Meperidine
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- Moderate to strong opiod agonist
- analgesic for moderate to severe pain - also used for Tourette's syndrome & restless leg syndrome - CYP2D6 metabolism into its active form (inhibited by SSRIs) - combined w/ aspirin to make percodan and w/ acetaminophen to make percoset - schedule II drug often abused |
Oxycodone
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- Moderate to strong opiod agonist
- Antitussive - generally given orally - can cause restlessness & hyperactivity - CYP2D6 metabolism into its active form (inhibited by SSRIs) - scheule II alone, III when combined w/ other drugs, IV in cough suppressants SE: - cause excitement/seizure in overdose CI: - small children |
Codeine
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- Moderate to strong opiod agonist
- CYP2D6 metabolism into its active form (inhibited by SSRIs) - combined with acetaminophen to make vicodin - Schedule II or III drug (often abused) - sometimes combined w/ homatropine to decrease abuse potential |
Hydrocodone
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- Partial opiod agonist at mu & kappa
- Low abuse potential - used for maintenance tx of opiod addiction because it decreases craving - won't work if injected when combined with naloxone (must be given sublingually) |
Buprenorphine
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- partial opiod agonist (competitive inhibition)
- Kappa receptor agonist but Mu partial agonist - less side effects than other opiods - Low abuse potential (schedule IV) |
Pentazocine
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- Miscellaneous opiod
- Mu receptor agonist - inhibits NE reuptake & stimulates alpha 2 receptors - used for moderate to severe pain but also approved for chronic & neuropathic pain - Schedule II drug SE: - nausea, vomiting, sedation |
Tapentadol
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- Miscellaneous opiod
- Weak Mu agonist - inhibits 5HT reuptake - good for mild to moderate pain - low abuse potential (not a scheduled drug) CI: - combo w/ antidepressants (siezures) - combo w/ MAOIs, TCAs, SSRIs can cause serotonin syndrome |
Tramadol
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- Pure opiod antagonist
- can reverse opiod side effects - must be injected (give till pupils dilate) - short duration of action (2 hours) - DOC: overdose of opiod |
Naloxone
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- Opiod antagonist
- used orally and long acting - used in alcohol recovery to decrease craving - will precipitate withdrawal - Liver toxidity w/ chronic use |
Naltrexone
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- Opiod antagonist
- peripheral acting mu opiod antagonist - Oral admin - indicated for tx of opiod induced constipation |
Alvimopan
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- can precipitate withdrawal in opiod dependent individuals
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Opiod antagonists
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- Opiod antagonist
- peripheral acting mu opiod antagonist - parenteral admin - indicated for tx of opiod induced constipation |
Methylnaltrexone
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- Opiod antagonist
- similar to naltrexone w/ slightly longer duration of action & less liver toxicity |
Nalmefene
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- Antitussive opiod
- not an analgesic - often combined w/ guafenisen (expectorant) - blocks NMDA receptors (abuse potential) - Decreases 5HT reuptake (seratonin syndrome if combined w/ MAOI) - OTC cough syrup & has become a drug of abuse in teens that has caused deaths CI: - never give with MAOI!! |
Dextromethorphan
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- Antidiarrheal opiod
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Loperamide
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- antidiarrheal used w/ opiods
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Diphenoxylate/atropine
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- inhaled agent used in anesthesia
- Analgesia, not anesthesia - euphoria - speeds induction of "2nd gas" - O2 given when it is stopped to prevent diffusion hypoxia - decreases hypotension - abused (dentists) SE: - peripheral neuropathy - megaloblastic anemia (WBC/RBCs) - nausea & vomiting common postop |
Nitrous Oxide
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- Inhaled anesthetic
- very soluble in blood - inhibits laryngospasm, cough - bronchodilator, used in asthma - normal anesthetic effects SE: - can cause Hepatitis - induces hepatic enzymes - increased intracranial pressure - sensitizes heart to catecholamines (can cause arrhythmia) - Miscarriage (occupational hazard) - malignant hypothermia (tx w/dantrolene) |
Halothane
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- Inhaled anesthetic
- too pungent for induction (airway irritation) - decrease BP SE: - increases intracranial pressure - increase HR |
Desflurane
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- inhaled anesthetic
- faster than halothane - no arrhythmia SE: - seizures - renal toxicity (contains fluoride ion) |
Enflurane (no pick)
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- used for maintenance of anesthesia
- depress neuronal activity - decrease excitatory transmission - facilitate inhibitory transmission - lipid soluble - potency proportional to lipid solubility (the more soluble the slower the induction & the less soluble the quicker the induction) - low MAC more potent - High MAC less potent |
Inhaled anesthetics
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- Inhaled anesthetic
- Easy to control depth of anesthesia - low airway irritation (good for induction) - safest in cardiovascular disease - DOC Anesthesia for children SE: - renal toxicity (contains fluoride ion) |
Sevoflurane
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- Inhaled anesthetic
- low toxicity - rapid induction & recovery - not good for induction - used in neurosurgery - DOC: general anesthesia SE: - can irritate airways - less intracranial pressure - increased heart rate |
Isoflurane
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- Barbiturate
- IV anesthetic used for induction - acts on GABA receptor - rarely used now cause there are better drugs CI: - porphyria |
Thiopental
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- IV anesthesia drug
- binds PCP on NMDA receptor - Dissociative anesthesia - sensation of floating - used with kids & animals - date rape & drug of abuse SE: - Emergence delirium in adults |
Ketamine
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- Rapid action
- used for induction of anesthesia - very lipid soluble - half life varies w/ duration of infusion |
IV anesthetics
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- IV anesthesia drug
- close to the perfect anesthetic in every way and anesthesiologists love it - facilitates GABA - Rapid induction/fast recovery - This & Midazolam are the m/c IV anesthesia drug - Least likely to cause vomiting - Lidocaine added for injection pain - Fospropofol is less painful prodrug - DOC for outpatient anesthesia SE: - Decreased cerebral blood flow, metabolism, intracranial pressure - injection site reaction possible - Respiratory depression (killed Michael Jackson) - allergic rxns due to emulsion (albumin) |
Propofol
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- IV anesthesia drug
- This & Propofol are the m/c IV anesthesia drug - acts on GABA receptor - used for short procedures in combo w/ opioid - amnesia reversed by flumazenil |
Midazolam
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- Strong opiod agonist
- effects reversed by naloxone - surgical drug (short surgical procedures w/ midazolam; & long surgical procedures because of good Cardiovascular profile) - used in lollipops & patches - high abuse potential - can cause truncal rigidity if given too fast - CYP3A4 metabolism |
Fentanyl
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- cause euphoria
- easy to use - Rapid onset & short action - potency & purity |
Abused drugs
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- Adrenergic stimulant
- CNS stimulant - local anesthetic (esther) - inhibits re-uptake of DA and NE - addicting (craving can be severe) - causes both psychological & physical dependence - can cause vasoconstriction - Bromocriptine decreases craving SE: - HTN, vasoconstriction, tachycardia - stroke in kids - increased temp - dilated pupils - bronchodilation - chronic use leads to reduction in overall brain activity - "bugs" itching & scratching at skin to get them out |
Cocaine as drug of abuse
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- "other" adrenergic stimulant
- CNS stimulant - Sympathomimetic that mimics epinephrine - MOA: Releases stored catecholamines, blocks reuptake - Stereotypic behavior - paranoia - delusions - hallucinations - psychosis - high abuse potential - changes "set point" in brain (more drug need just to feel ok Uses : narcolepsy, obesity, ADD SE: - tachycardia - HTN - psychosis Withdrawal - fatigue - increased appetite |
Amphetamines
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- CNS stimulant drug of abuse
- increases release of DA & NE in basal ganglia - More CNS effects than amphetamine w/ less peripheral - produces psychosis - chronic use leads to permanent neurotoxic damage - long term personality changes are common - Rapid physical & psychological dependence - "craving" in abstinence is intense - Cardiac toxicity can lead to pulmonary edema & heart failure SE: - seizures - organ damage - stroke - dental problems -"bugs" itching |
Methamphetamine
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- CNS stimulant
- activates nicotinic receptors in the CNS & periphery - increases 5HT & DA release - CNS effects (mild euphoria, increased arousal & appetite suppression) - VERY reinforcing & highly addictive - Buproprion used to tx cravings |
Nicotine as drug of abuse
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- Drug of abuse
- increases 5HT activity by blocking reuptake & stimulation 5HT receptors - increases blood pressure & heart rate SE: - hyperthermia - dehydration - kidney failure (can be fatal) - chronic use causes the serotonin neurons to atrophy and can result in long term deletion - persistent memory loss can occur |
MDMA "Ecstasy"
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- Drug of abuse
- binds to presynaptic cannabinoid receptors & inhibits release of glutamate & ACH - No physical dependence but psychological dependence is possible Medical uses - bronchodilation (asthma) - Antiemetic - Appetite stimulation (cancer) - analgesic - decreased spasticity/ataxia/muscle weakness (MS) - Decreased intraocular pressure (glaucoma) SE: - anxiety, decreased memory - Amotivational syndrome - Bronchial irritation (cancer risk) |
Marijuana
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- Drug of abuse
- synthetic cannbinoid receptor agonists - psychoactive effects |
Bath salts
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- drug of abuse
- GABA receptor weak agonist - used as date rape drug |
GHB
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- act on 5HT receptors in brain
- Euphoria & visual hallucinations - altered sense of time & reality - "bad trips" - Synesthesia (colors heard or sounds seen) - Don't cause dependence or stimulate DA pathways |
Hallucinogens (LSD, PCP, Mescaline)
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- NMDA receptor antagonist
- Developed as dissociative anesthetic - sensation of floating - produces analgesia accompanied by aggression - produces psychosis (tx w/ haloperidol in ER) - can cause coma w/ nonreactive pupils |
PCP (angel dust)
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- Weak bases (pKa of 8-9) that can cross cell membranes in their unionized form
- bind to & inactivate Na channels - high affinity for channels in activated (open) & inactivated states - lower affinity for resting (closed) states - Elevated Ca increases cell membrane potential and more channels are resting so block is diminished - elevated K depolarizes membrane leaving more channels inactivated so block is enhanced |
Local Anesthetics
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- Esther local anesthetic
- short acting - infiltration amnesia (injection into tissue) - Epidural anesthesia (injection into epidural space) - PABA is a metabolic product of it that inhibits action of sulfonamides - used for infiltration anesthesia & diagnostic nerve blocks - minimal systemic toxicity & no local irritation |
Procaine
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- ester type local anesthetic
- short acgint topical anesthesia of mucous membranes typically around the upper respiratory tract - inhibits Na channels - schedule II controlled substance SE: - blocks uptake of catecholamines at adrenergic nerve terminals CI: - HTN - CVD - Thyrotoxicosis - combo w/ other drugs that potentiate catecholamines |
Cocaine as a local anesthetic
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- local anesthetics
- shorter duration of action - increased systemic toxicity - metabolized by butryrylcholinesterase in plasma & liver |
Esther
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- Esterh local anesthetic
- only local anesthetic that isn't a weak base with a pKa between 8-9 - its pKa is 3.5 so it stays in an ionized form - this means it works in topical application only because it can't cross cell membranes in its ionized form - very lipohilic - used to tx minor burns (sunburn) SE: - methemoglobinemia |
Benzocaine
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- Esther local anesthetic
- long acting - slow onset (>10 min) - 10x more potent than procaine - Spinal anesthesia (injection into CSF) - opthalmological use |
Tetracaine
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- Amide local anesthetic
- intermediate acting - rapid onset - infiltration amnesia (injection into tissue) - Spinal anesthesia (injection into CSF) but transient neurological symptoms have been linked to this use of this drug - Epidural anesthesia (injection into epidural space) - DOC for local anesthesia infiltration blocks - also used as an antiarrhythmic agent |
Lidocaine as a local anesthetic
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- Amide local anesthetic
- inhibits butyrylcholinesterase - still used as topical - used for the dibucaine number test to differentiate individuals w. mutations & deficienies in their butyrylcholinesterase activity |
Dibucaine
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- Amide local anesthetic
- intermediate acting - highest rate of clearance of the amides - limited to use in dentistry SE: - metabolite may produce methemoglobinemia (excessive methemoglobin in blood turns you blue) that can be reversed w/ methylene blue CI: - cardiac or respiratory disease |
Prilocaine
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- Amide local anesthetic
- long acting - inverse differential block (motor block before or w/out sensory block) |
Etidocaine
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- Local anesthetics
- metabolized by CYP450 system in liver |
Amides
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- Amide local anesthetic
- long acting - more potent sensory block than motor block - infiltration amnesia (injection) - infiltration amnesia (injection into tissue) - Spinal anesthesia (injection into CSF) - Epidural anesthesia (injection into epidural space) - DOC: epidural during pregnancy & labor SE: - Cardiac toxicity (R enantiomers) |
Bupivacaine
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- Amide local anesthetic
- long acting - less lipid soluble & cleared more rapidly than bupivacaine - CYP3A4 metabolism - Less affinity for cardiac Na channels & thus less cardiac toxicity (S enantiomer of bupivacaine) - vasoconstricting effects at clinical doses |
Ropivacaine
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- amide local anesthetic
- intermediate acting - not used topically - not used in labor anesthesia |
Mepivacaine
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- analgesic
- antipyretic - lacks many of the side effects of aspirin - used for those with aspirin allergy - used for those w/ coagulation disorders - used for those w/ peptic ulcers - used w/ those being treated for gout - used in children - chronic alcohol consumption increases its toxicity (tx its toxicity w/ N-acetylcysteine) SE: - overdose causes fatal hepatic necrosis |
Acetaminophen
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- reversible inhibition of COX enzymes
- analgesic effect - Antipyretic effect - Anti inflammatory effect |
NSAIDs
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- Salicylic acid derivative but not metabolized to salicylic acid
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Diflunisal
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- MOA: irreversible inhibition of COX enzyme
- primary prevention of MI - prevents sensitization of pain recpetors - acts on hypothalamic area to reduce fever & malaise - doesn't work as analgesic in non inflamed painful conditions - slowly crosses BBB - low doses 1st order & high doeses 0 order Uses: - pain, antipyresis, antiinflammatory - MI, thrombosis prophylaxis - Long term used decreases colon cancer Effects - analgesic - antipyretic (lowers body temp in fevers only by resetting the thermostat) - anti-inflammatory - platelets SE: - respiratory/metabolic alkalosis/acidosis - Uric acid excretion decreased at low doses and enhanced at high doses - stomach irritation & gastric bleeding - Aspirin asthma (increased leukotriene synthesis - acute renal failure, interstitial nephritis CI: - dental procedures or surgery - gastric ulcer - liver/kidney damage - 3rd trimester of pregnancy - children (Reye's syndrome) |
Aspirin
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- Reversible COX2 inhibitor
- potential for less gastropathy & risk of GI bleeding - increased risk of cardiovascular disease CI: - GI disease - asthma - breast feeding - pregnancy - renal failure |
Celecoxib
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- Non specific reversible COX inhibitor
- Reduces PMN migration Very potent auto immune regulation agent w/ hight incidence of side effects -used for patent ductus arteriosus - DOC: Gout |
Indomethacin
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- Non specific reversible COX inhibitor
- Potent - decreases arachidonic acid bioavailability - Combined with Misoprostol to make Arthotec (decreases GI side effects) |
Diclofenac
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- Misoprostol + Diclofenac
- Diclofenac effects with less GI side effects |
Arthotec
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- Analgesia
- antipyrexia - anti inflammatory SE: - GI (pain, bleeding, ulcer, diarrhea) - pancreatitis - Bone marrow (agranulocytosis, aplastic anemia) - nephro & hepato toxicities - hypersensitivity |
Nonspecific reversible COX inhibitors
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- Non specific reversible COX inhibitor
- Prodrug w/ long half life |
Nabumetone
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- Non specific reversible COX inhibitor
- similar effects to aspirin - Long half life (13 hours) - Used to tx Gout |
Naproxen
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- Non specific reversible COX inhibitor
- analgesic used in post surgical pain - frequent GI side effects after 5 days of use - may be combined with opiods |
Ketorlac
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- Non specific reversible COX inhibitor
- drug of first choice - lowest incidence of side effects |
Ibuprofen
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- Non specific reversible COX inhibitor
- inhibits PMN migration & lymphocyte function - decreases O2 radical production |
Piroxicam
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- DMARD
- needed by T & B cells for purine synthesis - inhibits de novo lymphocyte purine synthesis - often combined with tacrolimus - don't give with antacids (block absorption) Side effects - skin rash - sepsis infection w/ CMV CI: - pregnancy/breast feeding - infection - active GI disease |
Mycophenolate
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- Used in cancer (antimetabolite) & immunosuppression (cell proliferation inhibitor)
- used to tx RA - does T cell & macrophage inhibition - Leukovorin is the antidote to methotrexate toxicity MOA: inhibits dihydrofolate reductase to block DNA, RNA & protein synthesis SE: - precipitates in renal tubules (hydrate!!) - hepatotoxicity (long term use) - alopecia - BM suppression - teratogen, sterility |
Methotrexate
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- DMARD
- Interleukin 1 receptor antagonist |
Anakinra
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- DMARD
- inhibits pyrimidine synthesis - inhibits induction of COX 2 - used for RA SE: - nephro & hepato toxicity - oral ulceration - abdominal/back pain CI: - pregnancy/breastfeeding - liver or renal failure |
Leflunomide
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- DMARD
- Chelating drug effective in Rheumatoid arthritis & Wilson's disease - DOC: copper chelation SE: - pruritis, rash, alterations in taste - thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia - Lupus like disease - Goodpasture's syndrome, myasthenia gravis, polymyositis, stenosing alveolitis |
Penicillamine
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- DMARD
- fully human recombinant fusion protein - signal blocker of T cell activation - CD80 & 86 |
Abatacept
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- DMARD
- has antihistaminic, anticholinesterase & antiprotease properties - inhibits PG synthesis - inhibits biosynthesis of mucopolysaccharide - stabilizes lysosomes SE: - pruritus - hemolysis (G6PD deficient) - ototoxicity - Retinopathy, - peripheral neruopathy |
Hydroxychloroquine
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- DMARD
- dimeric fusion protein - targets TNF receptor on IgG to inhibit TNF SE: - injection site rxn - infections - increased incidence of antibody formation CI: - bone marrow suppression - pregnancy/breast feeding/children - Diabeties - infection - sepsis - varicella |
Etanercept
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- DMARD
- chimeric monoclona antibody targeted agsint TNF alpha - approved for Crohn's disease & RA - combined w/ methotrexate - IV SE: - head ache - infusion rxn CI: - pregnancy/breast feeding - kids - infection |
Infliximab
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- DMARD
- Recombinant IgG monoclonal antibody - specific for TNF alpha - unlike infliximab it is approved for monotherapy tx of RA SE: - rash - flu like symptoms - head ache - pruritus - nausea/vomiting |
Adalimumab
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- DMARD
- chimeric murine/human monoclonal antibody - binds to CD20 B lymphocyte antigen - used to tx non Hodgkins lymphoma - also used in chronic lymphocytic leukemia |
Rituximab
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- DMARD
- used to tx RA - as effective as penicillamine & less toxic - recommended you monitor for hepatitis & blood dyscrasias for 2-3 works of first 3 months of tx, then less frequently therafter SE: - GI disturbances - rash |
Sulfasalazine
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- Gout drug for acute attacks
- no analgesic effect - binds tubulin to inhibit microtuble assembly - anti-inflammatory effect by inhibiting leukocyte migration & phagocytosis SE: - one of the 5 major diarrhea drugs - Nausea & vomiting, abdominal pain |
Colchicine (no picture)
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- long term tx of Gout
- Keep urine pH above 6 - can trigger stone formation in patients excreting large amounts of uric acid - initial administration may trigger gouty attack so prophylactic colchicine therapy may be needed SE: - GI irritation |
Uricosuric agents
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- uricosuric agent for long term tx of gout
- therapy shouldn't be started for 2-3 weeks following acute attack - decreases excretion of many acidid compound metabolites |
Probenacid
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- inhibit xanthin oxidase to inhibit the synthesis of uric acid
- effective at tx primary & 2ndry forms of gout - initial therapy may provoke acut gouty attack SE: - vasculitis - agranulocytosis - hypersensitivity |
Xanthine oxidase inhibitors (Allopurinol & Febuxostat)
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- Recombinant form of urate oxidase
- since it is a foreign protein you can only use it once, and the next time the patient will have a rxn to it - urate oxidase metabolizes uric acid into allantoin SE: - tumor lysis syndrome (patients w/ malignancies or solid tumors) - severe hypersensitivity |
Rasburicase
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- Migraine tx drug
- symptomatic tx for migraines - 5HT agonist - DOC: Migraine SE: - coronary vasospasm, arrhythmia, angina, MI, cardiac arrest - CVA, seizure, intracranial bleeding - peripheral vascular ischemia, bowel ischemia CI: - pregnancy, breast feeding - hx of seizures - renal impairment - smoking - cardiac disease - cerebrovascular disease - diabetes |
Sumatriptan
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- partial 5HT agonist for migraine tx
- partial agonist on alpha receptors - similar mechanism to triptans but less specific - big gun for shooting down migraines SE: - nausea, vomiting - cardiovascluar toxicity - ergotism (vasoconstriction + CNS) CI: - Thromboangitis obliterans or thrombophlebitis - atherosclerosis - severe HTN - allergy - pregnancy - peptic ulcers - renal or hepatic diseaese |
Ergotamine tartrate
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- beta blocker used in migraine prophylaxis
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Propanol
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- Ca channel blocker used in migraine prophylaxis
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Verapamil
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- ARB used in migraine prophylaxis
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Losartan
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- TCA used in migraine prophylaxis
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Amitriptyline
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- Muscle relaxant used in migraine prophylaxis
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Botulinum toxin
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- anticonvulsants used in migraine prophylaxis
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Valproic acid & topiramate
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- Alpha2 agonist used for migraine prophylaxis
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Clonidine
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