-caine
local anesthetic
-coxib
cyclooxygenase (COX)-2 inhibitors (eg, celecoxib)...inhibit inflammation and pain, different than NSAIDs which block COX-1 AND COX-2, common for arthritis
-dipine
dihydropyridine calcium channel blockers (eg, nifedipine)...these relax the muscles of heart and blood vessels, treating angina and hypertension, think "pine tree"=relaxed, de-stressed
-dronate
bisphosphonate (eg, alendronate, Fosamax)...treats osteoporosis or Paget's Disease, could cause bisphosphonate-associated osteonecrosis of the jaw, think about an old woman with osteoporosis flying a drone
-fungin
glucan synthesis inhibitor, antifungal (eg, caspofungin)...can treat a candida infection in the blood
-gliptin
dipeptidyl peptidase-4 (DPP-4) inhibitor drug for type 2 diabetes (eg, sitagliptin)...lowers blood sugar, think about a diabetic patient drinking LIPTON sugary tea and needing this drug
-glitazone
peroxisome proliferator activated receptor gamma (PPAR-gamma) activator for type 2 diabetes (eg pioglitazone), think about a diabetic patient eating a calZONE and needing this drug
-grel
P2Y12 adenosine diphosphate (ADP) receptor inhibitor in platelets (eg, clopidogrel, Plavix)
-prevents heart attack and stroke, makes patients more susceptible to bleeding and bruising
-think "grel"="gel". this is an anti-gel for platelets.
-olol
beta-adrenergic receptor blocker (eg, propranolol)
-treats arrythmia, protects heart from second heart attack, treats hypertension
-"olol" looks like two backwards b's for beta-blocker
-ilol" or "-alol
beta-adrenergic receptor blocker that also blocks alpha-1-adrenergic receptors (eg, carvedilol)....by blocking the alpha-1 receptors, it causes vasodilation of skin/brain vessels
-mab
monoclonal antibodies (eg, infliximab)
-works against TNF-alpha (part of immune reaction) to treat autoimmune diseases
-can treat rheumatoid arthritis, ankylosing spondylitis, Crohn's disease, plaque psoriasis, and ulcerative colitis.
-onium" or "-urium
quaternary ammonium compounds, usually competitive, peripherally acting skeletal muscle relaxers (eg, pancuronium)
-binds nicotinic acetylcholine receptor at neuromuscular junction which prevents acetylocholine from binding
-osin
alpha-1-adrenergic receptor blockers (eg, prazosin)
-vasodilation of skin and GI tract smooth muscle
-think of a devil "sinning" by being lazy and laying on the couch digesting a bag of Doritos
-oxacin
fluoroquinolone antibacterial (eg, moxifloxacin)
-may treat pneumonia, sinusitis
-think of an "ox" that has pneumonia
-parin
heparin or low molecular weight heparin (eg, tinzaparin)
-treats deep vein thrombosis and pulmonary embolism
-prazole
proton pump inhibitor (eg, esomeprazole)
-"omeprazole"= Omesec, Prilosec
-treats heartburn, damaged esophagus, stomach ulcers, gastroesophogeal reflux disease (GERD)
-think "get a prize" for not having heartburn
-penem
carbapenem beta-lactam antibacterial (eg, ertapenem)
-treats pneumonia and urinary tract, skin, diabetic foot, gynecological, pelvic, and abdominal infections that are caused by bacteria
-"penem" sounds like "PNEUMonia
-pril" or "-prilat
angiotensin-converting enzyme (ACE) inhibitors (eg, captopril)
-can treat high blood pressure and heart failure
-think "ACE", play cards in A
pril
-sartan
angiotensin II receptor blockers (eg, losartan)
-treats high blood pressure
-think "sartan"="satan"= gives you high BP
-statin
3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor antilipid drugs (eg, lovastatin)
-reduces levels of cholesterol
-teplase
tissue plasminogen activator drug (eg, alteplase)
-breaks down blood clots
Cell surface receptor types
-G protein linked receptors (7 plasma membrane domain)
-Ion channel receptors
-Transmembrane receptors (with cytosolic enzyme domains)
-Intracellular nuclear receptors that alter gene expression
-Cell surface adhesion receptors
Type 1 dose response curves are ___________, and useful for determining characteristics of _____________ and ____________.
Graded, agonists, antagonists
The maximal effect of a drug
Intrinsic activity
The effect of a drug as a function of level of binding to its receptor
Efficacy
-The attractiveness of a drug to its receptor
-Measured by the dissociation constant, Kd
Affinity
The lower the Kd, the [lower/higher] the affinity
Higher
-The response to a drug over a given range of concentrations
-Measured by the effective concentration of the drug leading to its half maximal effect, EC50
Potency
The effective concentration of a drug leading to its half maximal effect
EC50
-These type of drugs have intrinsic activity
-They elicit a response from the tissue
Agonists
These type of drugs have no intrinsic activity
They do not elicit a "graded response" alone
Antagonists
The y-axis of a Type 1 graded dose response curve
Graded response %
Type 2 Dose Response Curve
Quantal
Y axis of Type 2 Dose Response curve
Quantity of subjects responding to a drug
Therapeutic index
Ld50/Ed50
An estimate of the margin of safety for a drug
Weak acids tend to concentrate in areas of low/high pH
High pH
Think weak acid, strong base
Weak bases tend to concentrate in areas of low/high pH
Low pH
Think strong acid/weak base
Weak acids are excreted more rapidly at lower/higher pH because they are concentrated in the ____________ of the kidney tubule
Higher, lumen
A drug made active by metabolism
Prodrug
Phase reaction of drug metabolism involving oxidation, reduction, hydrolysis
Phase 1
Phase reaction of drug metabolism involving conjugation, in which a substituent is added to a drug. The most common type is glucuronide conjugation.
Phase 2
Most metabolism of drugs occurs in the ________, and can be microsomal or nonmicrosomal.
Liver
Three types of excretion in the kidney
Glomerular filtration, active tubular secretion, passive tubular transfer (from blood to lumen or lumen to blood (reabsorption)).
k * t1/2
First order Rate constant * half time
0.693
Cp0 * Vd
Concentration in plasma at time 0 * volume of distribution
Dose
k * Vd
First order rate constant * volume of distribution
Clearance
If the same mg of a drug are eliminated every hour, independent of the concentration, this is ________ order kinetics
Zero
If the same fraction of a drug is eliminated every hour which Is proportional to the drug's concentration, this is _______ order kinetics
First
-Transporter responsible for reducing a drug's accumulation
-Found in the liver
P-glycoprotein
-Enzyme in liver that does metabolism
-microsomal
Cytochrome P-450
Induction/inhibition of metabolism is a reaction to certain drugs by which the # of liver cytochrome enzymes increases, resulting in an increase/decrease in effect of other drug
Induction, decrease
Induction/inhibition of metabolism is a reaction to certain drugs by which one drug either competes for metabolism of another or directly inhibits metabolizing enzymes
Inhibition (could also inhibit P-glycoprotein transporters)
The rate of metabolism is dictated by the ________________ isozyme profile of the patient
Cytochrome p-450
An adverse effect that occurs within the therapeutic Dose range of the drug
Side effect
-An adverse drug reaction that is due to a genetic change usually involving a change in enzyme activity
-occur rarely in population
-could be an allergy or sensitivity
Idiosyncratic reaction
If a pt is taking itroconazole (anti fungal), clarithromycin (abx for skin and respiratory system), or a cytochrome P-450 inhibitor , what dental drugs could interact?
diazepam (Valium) or triazolam (Halcion) (increased sedation due to reduced metabolism of benzodiazepines)
If a pt isn't taking antacids, what dental drug might be affected?
Tetracycline (commonly treats acne or bacterial infections) (reduced absorption of tetracycline)
If a pt is taking anticoagulants (Heparin, warfarin), what dental drug should be used with caution?
Aspirin (increased bleeding tendency)
If a pt is taking probenecid (reduces Uric acid with gout), what dental drug can decrease the effect of Probenecid?
Aspirin
If a person is taking methotrexate (immunosuppressive drug for cancer, arthritis, or psoriasis), what dental drug could cause increased methotrexate toxicity?
Aspirin
If a person is a chronic alcoholic, which dental drug could cause increased liver toxicity?
Acetaminophen (Tylenol)
if a pt is taking cholinesterase inhibitors (these inhibit breakdown of ACh, thereby increasing neuromuscular transmission for myasthenia gravis), what dental drug should be used with caution?
Local anesthetic (these reduce the ACh inhibitor effect)
The rate of drug metabolism can vary greatly, depending on the _______________ isozyme profile of the pt.
Cytochrome P-450
If a pt has a genetic condition of
NADH-methemoglobin reductase deficiency
, which 2 anesthetics do you want to avoid that could cause methemoglobinemia?
Benzocaine, prilocaine
If a pt has a genetic condition of
G6P dehydrogenase deficiency
, which 3 drugs do you want to avoid that could cause a response of hemolytic anemia?
Aspirin, primaquine (treats, prevents malaria), sulfonamides (antimicrobials)
If a pt has a genetic condition of
abnormal heme synthesis
, which drugs do you want to avoid that could induce porphyria (build-up of red blood cell proteins)?
Barbiturates (sedatives, anxiolytics, anticonvulsants), sulfonamides (antimicrobials)
If a pt has a genetic condition of
low plasma cholinesterase activity
, which anesthetic do you want to avoid which could cause local anesthetic toxicity?
Procaine (and other ester local anesthetics)
If a pt has a genetic condition of
altered muscle calcium homeostasis
, which type of anesthetics (2) do you want to avoid which could cause malignant hyperthermia?
Volatile inhalation anesthetics, succinylcholine (causes paralysis for general anesthesia)
If a pt has a
prolonged Q-T interval
genetic condition, which 2 classes of drugs do you want to avoid which could cause "Torsades de pointes" (tachycardia)?
Antipsychotics, antiarrhythmics
Drug testing phase (I-IV) that uses normal volunteers, and assess safety and pharmacokinetics.
Phase I
Drug testing phase (I-IV) that uses patients who could benefit from the drug. Assesses
clinical efficacy
, pharmacokinetics, and safety.
Phase II
Drug testing phase (I-IV) that uses a larger # of pts, involving several medical centers. Safety and clinical efficacy are assessed.
Phase III
Drug testing phase (I-IV) that is post-marketing surveillance. Safety, patterns of use, and new indications are assessed.
Phase IV
What are the risk categories of drugs with pregnancy, from the safest to the most risk for fetuses?
A, B, C, D, X
Which act in 1906 forbade the adulteration and mislabeling of drugs?
Pure Food and Drug Act
Which act regulated opiates and cocaine in 1914?
Harrison Narcotic Act
Which act mandated the safety of drugs and the role of FDA in enforcing safety in 1938?
Food, Drug, and Cosmetic Act
Which act used restrictions for certain drugs by prescription only in 1952?
Durham-Humphrey Act
Which act provided incentives for developing drugs for rare diseases in 1983?
Orphan Drug Amendment
Which act in 1997 replaced "legend" with label "Rx only",
-allowed manufacturer to discuss off-label uses of drugs with practitioners
-revised accelerated track approval for drugs that treat life-threatening disorders
-made provisions for pediatric drug r
FDA Modernization Act
Which 2005 act established new regulations for sale of ephedrine, pseudoephedrine, and phenylpropanolamine ?
Combat Methamphetamine Epidemic Act
In the somatic nervous system, the nerve goes from the CNS to striated muscle. Which neurotransmitter acts on striated muscle?
ACh
In the sympathetic division of the autonomic nervous system, the path is:
CNS ------------> ACh-nicotinic (ganglion) ------------> What is final neurotransmitter for
heart, smooth muscle, glands
NE
CNS -----------> ACh-nicotinic (ganglion) ------------> What is final neurotransmitter for the muscarinic site of
sweat glands and some blood vessels
?
ACh (muscarinic)
CNS --------->ACh-nicotinic (adrenal medulla) ----------->what is made at the adrenal medulla?
epinephrine, norepinephrine
In the parasympathetic division:
CNS ---------> ACh-nicotinic (ganglion) --------------> ACh (is this a nicotinic or muscarinic site?)
Muscarinic (heart, smooth muscle, glands)