24. Pharmacology: Part II (Narcotics-Non narcotics) Flashcards
Gold standard of narcotics
Morphine
Narcotics are derived from what type of plant?
Poppy plant : Papaver somniferum
Narcotics are also known as (3Os)
Opioids
Opiates
Opium
3 receptors of narcotics
Mu
Kappa
Delta
Drugs with morphine-like properties that acts in CNS
Morphine
Opioid receptors (mu kappa delta) nakikita sa: Limbic system (emotion center)
- Narcotics = controls pain and reaction to pain
: (because inaalter ung limbic system)
Limbic system: 🔺Hippocampus - memory center 🔺Amygdala - resp for fear,anger, arousal; (almond shape) 🔺substantia nigra - dopamine production 🔺basal ganglia - voluntary motor movts
Most common side effect of narcotics
Nausea
- (Area Postrema)
Part of nervous system that controls
✅cough reflex
✅gastric motility
📌 action of narcotics???
Solitary nuclei - gag,cough reflex..
📌 Narcotics suppresses cough reflex
Narcotics that suppresses Cough reflex
“anti tussive” (Dextromethorphan)
Drug taken to inhibit gastric motility
Loperamide (Diatabs)
BQ: “gate” in gate control theory
Substantia gelatinosa of Rolando
Most accepted theory for pain;
- painful stimulus: gate opens
- non painful: gates closes
Gate control theory
BQ: What are the endogenous opioids produced by our body?
Enkephalins
Endorphins
BQ: Narcotic agents blocks pain in the “peripheral” nervous system. True/False?
False - blocks pain in CNS!
BQ: What is the combination of Diphenoxylate and Atropine
Lomotil
Induces gastric motility
Laxatives (Bisacodyl)
Therapeutic effects of Narcotics: (ASEE)
Analgesia
Euphoria
Sedation
Eliminates cough
BQ: what kind of drug is Guaifenesin?
Expectorant
Most common side effect of narcotics
Nausea
BQ: drug that puts patient in “trans like state”
Ketamine
Adverse effect of narcotics which is opposite of euphoria
Dysphoria
Most serious side effect of narcotics
Respiratory depression
BQ: Morphine Triad (due to overdose)
Miosis (pupillary constriction:pinpoint)
Respiratory depression
Coma
BQ: What are the components of Neuroleptic analgesia? (Anesthetic technique that puts px in stage 1 anesthesia)
- neuroleptic agents/antipsychotics
- Butyrophenones : (induces hallucinations) - Narcotics
- Nitrous oxide (optional)
BQ: What is the drug that causes “dissociative” anesthesia? / “trans like state”
Ketamine
- conscious mind separated from body
- “trans like state”
BQ: What type of drugs are contraindicated to glaucoma
Diazepam
Anticholinergic drugs
Ano nakikita ng patient na may glaucoma?
“Tunnel vision”
BQ: type of NARCOTIC drug contraindicated to glaucoma?
Meperidine (may slight anticholinergic effect)
BQ: Drug contraindicated to glaucoma
choices: one of “DiTriBeAM” bec it has slight anticholinergic
Is Diphenhydramine contraindicated to glaucoma? Yes. (All DiTriBeAM sa boards)
Drug used for severe orofacial pain
Codeine
- “prodrug” : converted to morphine
- orally
- common na ginagamit sa dental: bec low drug dependence
Acetaminophen is similar with what drug in ph
Acetaminophen : Paracetamol
Tylenol ~~~~~~~ Biogesic
Other term for acetaminophen
“APAP”
N-acetyl paraminophenol
Oxycodone + Acetaminophen = what brand name?
“Tylox”
“Percocet”
Oxycodone
“Molly”
Ecstasy
What is the route of administration of morphine and meperidine
Parenteral (IV)
More potent than morphine
Fentanyl
BQ: “Diacetylmorphine”
Heroin
BQ: strip name of drugs
- “Horse”
- “Big H”
- “Brown sugar”
Heroin
Strip name of cocaine
Coke
Candy
“Poor man’s cocaine”
Shabu/meth/crystals
Methamphetamine HCl
Dental disease assoc with Methamphetamine HCl
“Meth mouth”
- Meth = enhances sympathetic nervous system
- Saliva during symp = ⬇️ = Xerostomia ➡️ Caries and Perio dse = METH MOUTH!!!
Strip name of “MJ” / “Weed” / “Blunt”
Marijuana (Cannabis sativa)
BQ: Drug that shouldnt be combined with MAO-Inhibitors
Meperidine
BQ: Narcotic antagonists
Naloxone
“naltrexone” : pag wala sa choices ung naloxone
BQ: Give 4 drugs that are associated with respiratory depression and dependence
"SNAB" Sedative hypnotics Narcotics Alcohol Benzodiazepines
BQ: “non schedules narcotic” (no prescription needed)
Tramadol
BQ: Drugs with different classification
Opioid/Non opioid
Tramadol
Propoxyphene (Darvon)
Pentazocine (Talwin)
BQ: Some narcotics(depressant) that are metabolized to a CNS stimulant by the LIVER
Meperidine (Demerol) ➡️ “nor”meperidine
Propoxyphene (Darvon) ➡️ “nor”propoxyphene
BQ: Study SCHEDULE II drugs : HIGH potential for abuse or dependence
- Hydromorphone (Dilaudid)
- methadone (Dolophine)
- Meperidine (Demerol)
- Oxycodone (percocet)
- fentanyl (sublimaze, duragesic)
- Morphine
- Opium
- Codeine
BQ: Impaired control over taking the drug
Pag nasa isip mo ung drug
Psychic dependence
Continued administration of the drug is required to prevent unpleasant “withdrawal syndromes” ✅ (Ex. Alcoholic, smokers)
- “hinahanap ng body mo yung drug”
Physical dependence
BQ: Increasingly large dose of narcotics are required to produce the same degree of analgesia (Ex. Caffeine)
Tolerance
BQ: Opioid withdrawal: Life threatening or not?
Not life threatening
Most common drug assoc with withdrawal symptoms
Alcohol (life threatening)
4 na kailangan para makapag induce ng General anesthesia = which results to COMA
Sedation
Amnesia
Muscle paralysis
Analgesia
Stage na delikado or critical sa patient
Stage 2
- dapat maging stage 3 na agad
- uses FAST ACTING / Ultrashort
End of stage 1 and start of stage 2
Unconsciousness
Desirable stage during GA
Stage 3
Guerin’s stages of General Anesthesia
Stage 1 - Amnesia and analgesia
Stage 2 - Excitement and Delirium
Stage 3 - Surgical anesthesia
Stage 4 - Medullary Paralysis
Inhalational drugs used in GA
Halothane
Desflurane
Short acting hypnotic agent
Propofol
Used for dissociative anesthesia
Ketamine (trans like state)
Blocks pain mainly in the PERIPHERAL NERVOUS SYSTEM
- Doesn’t have CNS depression effects
- Doesn’t act in Opioid receptors
Non narcotic analgesics
Non narcotic analgesics
Acetaminophen
Aspirin
NSAIDS
General pharmacological effects of Non narcotics
Mild to mod pain
Controls fever / antipyretic
Anti inflammatory
Non narcotic analgesics block what enzyme resulting to decrease prostaglandin production
Cyclooxygenase
BQ: Prostaglandins produced in CNS causes:
Fever and pain
BQ: Prostaglandins produced in PNS causes:
Pain
Inflammation (vasodilation)
Gastric protection
Enzyme that breaksdown PHOSPHOLIPID BILAYER during tissue damage
Phospholipase A2
Breakdown of Phospholipid bilayer by Phospholipase A2 results to production of what chemical?
Arachidonic acid
Once arachidonic acid goes to the RESPIRATORY SYSTEM, It will bind to what enzyme?
Lipooxygenase
Arachidonic acid + Lipooxygenase =
Production of LEUKOTRIENES
Binding site of Leukotrienes
Leukotriene-Receptor sa Lungs
Binding of Leukotrienes to Leukotriene-receptor sa lungs = it will result to?
Bronchoconstriction
- main reason kaya nagkaka-ASTHMA
Drug that inhibits “lipooxygenase pathway”
✅ It creates a barrier = so that Leukotrienes can’t bind to the receptors.
✅ prevents Bronchoconstriction
Leukotriene receptor blocker
BQ: Example of a “Leukotriene receptor blocker” that prevents ASTHMA
Montelukast
If yung Arachidonic acid nakarating sa CNS - it will meet what enzyme?
COX2
COX2 in CNS converts AA into:
Prostaglandins: (pain and fever)
COX1 in PNS converts AA into:
Thromboxane A2 (platelets: blot clotting)
Prostaglandins
- protects stomach
- Inc renal blood flow
Prostaglandin that protects stomach and increases renal blood flow is derived from?
AA + “COX1” in PNS
COX2 in PNS converts AA into:
Prostaglandins
- pain
- inflammation (vasodilation=inc blood flow)
Prostacyclins
- inflammation/swelling
Enzyme responsible pag nagkakaroon ng WOUND
COX2 of PNS
Converts AA into Prostaglandins and Prostacyclins = pain and inflammation
Produced mainly by platelets: Helps in blood clotting
Thromboxane A2
BQ: What are the 3 end products of cyclooxygenase pathway?
Thromboxane A2
Prostaglandins
Prostacyclins
BQ: An Exception: CENTRALLY ACTING Non-narcotic analgesic
non narcotic=PNS acting
Acetaminophen
Acetaminophen inhibits what enzyme?
Cyclooxygenase (COX2 in CNS)
-inhibits pain and fever
Is acetaminophen/paracetamol an NSAID?
No. Not an NSAID!
- bec it doesnt have an anti inflammatory effect/ doesnt control swelling
Centrally acting analgesics
Narcotic analgesics
Peripherally acting analgesics
Non-narcotic analgesics
{*except: ACETAMINOPHEN}
NSAIDS acts on CNS/PNS???
Nsaids - PNS
NSAIDS inhibits what enzymes?
Cox1 and Cox2 in PNS
Toxic effects of NSAIDS
- “reduces formation of blood clot” (TXA2)
- “gastric irritation/ulcers” (removes prostaglandins that protects stomach)
- “kidney damage” (removes prostaglandins na nagiincrease ng renal blood flow)
Therapeutic effects of NSAIDS
Anti-inflammatory
Analgesic
(-inhibits prostaglandins and prostacyclins)
Aspirin is an active or inactive drug?
Inactive / “prodrug”
- converted to SALICYLATES
Aspirin: CNS/PNS?
Peripherally acting drug
BQ: Side effect of aspirin pag binigay sa child with viral infection
Reye’s syndrome
Viral inf presents “fever”: Aspirin has mild effects on CNS kaya mej anti pyretic dati!now anticoagulant na!
Is Aspirin sometimes classified as “NSAID”?
Yes: Aspirin = NSAID ✅
Has mild anti inflammatory effect
BQ: MOA of aspirin? Why is ASPIRIN used as a “blood thinner” or “anticoagulant”?
Aspirin “IRREVERSIBLY blocks COX1”
(Platelets uses COX1 to produce TXA2)
ASPIRIN kahit wala na sa body: causes platelets to be permanently damaged or non functional=hindi na makakaproduce ng TxA2 which is resp for blot clotting = Kaya ginagamit sya as anticoagulant but lasts only until 10 days (lifespan ng platelets)
- Unlike sa NSAIDS: Once na nawala NSAID sa body (after 4hrs): platelets will restore cox1 = can produce TXA2 again
BQ: How many days prior to surgery must the patient stop taking Aspirin?
7 days (stop!)
NSAIDS that selectively blocks COX 2
COX 2-inhibitors
*Cox2 lang iniinhibit therefore:
Cox1❌: No adverse effects: gastric irritation, renal damage, inc bleeding tendency
Drug examples of Cox2-inhibitors
Celecoxib
Etoricoxib (Arcoxia)
Valdecoxib
BQ: which of the ffg drugs na wag ibibigay sa patient prior to surgery?
NSAID (ung nasa choices)
specifically: Aspirin dapat: but aspirin is considered a NSAID
(Nsaids like mefenamic acid ok lang ibigay before surgery)
Only non narcotic analgesic WITHOUT anti inflammatory effects
Acetaminophen
- no anti inflammatory effect bec: Centrally acting
- anti pyretic and analgesic only
3 drugs that are HEPATOTOXIC (“Hart”)
Hepatotoxic:
- Acetaminophen
- Rifampicin
- Tetracyclines
“Overdose of aspirin”
Salicylism
Toxic effects of ASPIRIN:
✅gastric irritation: ❌cox1:prostaglandins
✅renal damage: ❌cox1:prostaglandins
✅salicylism: overdose
✅prevents clotting: ❌cox1:txa2
✅Reye’s syndrome - if aspirin is given to a child with viral infection
Aspirin and other NSAIDS can enhance the effects of
Warfarin(Coumadin) and Coumarin
*wag icocombine: anticoagulant + anticoagulant = BLEEDING!!!!!
BQ: Drug used to treat Salicylism?
Sodium bicarbonate
BQ: What is the parent drug that is converted to acetaminophen?
Phenacetin
BQ: Excessive doses of these 2 drugs can lead to “Narcotic-like” adverse effects
Pentazocine
Propoxyphene
BQ: Drug interaction of PNS acting and CNS acting Non-narcotic analgesics
Pns + Cns non-narcotic analgesic are SYNERGISTIC!!! (1+1=>2)
Example: Ibuprofen(nsaid:pns) + Paracetamol(cns) = Alaxan
Non scheduled drug: dont need prescription
Tramadol
NSAID + another NSAID cannot be combined ❌
⬆️⬆️ Toxic effects!!!!
✅ Nsaid + Paracetamol = Synergistic
Brand name of Ibuprofen
Alaxan, medicol, midol
Generic name of flanax
Naproxen
Examples of NSAIDS:
Ibuprofen Naproxen Diclofenac Mefenamic acid Sulindac Piroxicam Oxaprozin Indomethacin Nabumetone
Toxic effects of COX2-inhibitors
Can lead to heart attack or stroke or any cardiac disease
{explanation:}
Wall of bv is made up of Prostacyclin and TxA2
Cox2-inhibitors inhibits Prostacyclins; Magdodominate TxA2⬆️=constricted BV dahil lumalapot yung blood: ⬆️obstruction
Ideally: Cox2-inhibitors are taken maximum of how many days
Maximum of 7 days
NSAIDS that reduces pain, fever(minor), and inflammation WITHOUT having GI problems
Cox2-inhibitors