Drugs Flashcards
Heparin affects what clotting factors
II (Prothrombin) and X (Stuart-Factor)
It binds to antithrombin III to increase activity
Heparin
Antidote for Heparin
Protamine sulfate
What clotting factors does warfarin affect?
Vit K-dependent: II (prothrombin), VII (Stable factor), IX (Christmas factor, X (Stuart factor)
Antidote for warfarin
Vitamin K
Treatment for tic douloureux
Carbamazepine (Tegretol)
Antiepileptic drugs (2)
Benzodiazepine - diazepam
Diphenylhydantoin - phenytoin
Drug contraindicated for hyperthyroidism
Epinephrine. May cause thyroid storm
Drugs for hyperthyroidism
Propythiouracil (PTU)
Methimazole
Drug for hypothyroidism
Levothyroxine (synthethic thyroxine)
tx for anaphylaxis
epi
adult dose: 0.5mL of 1:1000 or 0.5mg of epi
pedia dose: 0.01mg/kg (max dose 0.3mg)
Vancomycin side effect
Red man syndrome
Tx for TB
RIPES / StRIPE
Rifampicin
Isoniazid (1st line, most hepatotoxic)
Pyrizinamide
Ethambutol
Streptomycin (ototoxic)
Tx for hansen’s disease
Aka leprosy (Mycobacterium leprae)
Rifampin + dapsone (sulfone/sulfonamide)
content of artificial tears and artificial saliva
artificial tears - hydroxypropyl cellulose
artificial saliva - hydroxymethyl cellulose
tx for sjogren’s syndrome
- immunosuppressant drugs such as
-cyclosporine,
-corticosteroids (also an anti-inflammatory) - cholinergic drugs (parasympathomimetic agents) - pilocarpine
tx for toxicities
activated charcoal
syrup of ipecac
gastric lavage (deposit then aspirate)
cathartics (laxative)
most important liver microsomal enzyme because it metabolizes most drugs
cytochrome p450
plasma enzyme important for metabolizing drugs
plasma pseudocholinesterase metabolizes esters and succinylcholine
bypasses metabolism stage of pharmacokinetics? bypass absorption?
bypass absorption - IV route
bypass metabolism - nitrous oxide
double i na anes but ester?
amide na sa both sa liver and plasma namemetabolize?
piperocaine - ester
articaine - amide but sa both metabolized
Tx for amoebiasis
Antiprotozoal and antibiotics
Co-trimoxazole (bactrim) - trimethoprim + sulfamethoxazole
Or
Metronidazole (anaerobes only)
Tx for malaria
Doxycycline
Quinine analog (mefloquine)
Primaquine
Chloroquine
“#1clean queen”
Tx for angina pectoris
Nitrates.
Nitroglycerin (sublingual)
Amyl nitrate (inhalation drug)
antibiotic prophylaxis (recommended dose)
30-60mins before invasive procedure
Amoxicillin (oral and parenteral) - 2g (Adult), 50mg/kg (child)
ampicillin (parenteral) - 2g (A), 50mg/kg (C)
cefalexin (oral and parenteral) - 2g (A), 50mg/kg (C)
azithromycin and clarithromycin (oral and parenteral) - 500mg (A), 15mg/kg (C)
*clindamycin (oral and parenteral) - 600mg (A), 20mg/kg (C)
*not recommended according to ADA 2021
Time required for a drug to reduce half of its initial value
Half-life
Rate at which the active drug is removed from the body
Clearance rate
Differentiate zero-order kinetics and first-order kinetics
Zero-order = clearance rate is constant and is not dependent on concentration of drug in plasma fluid
First-order = clearance rate is dependent on the concentration of drug. Half life ang constant
Drugs that follow zero-order have higher chance to accumulate in the body
Amount of drug eliminated is dependent on the concentration of drug in the plasma fluid
First-order kinetics
Amount of drug eliminated is constant and not dependent on the concentration of drug in the plasma fluid
Zero-order kinetics
Free-floating drugs in the plasma fluid?
Drugs attached to plasma protein?
Free-ionized drug
Bound drug (reservoir of free-ionized)
Phenomenon of drug metabolism whereby the concentration of orally taken drugs is reduced before reaching the systemic circulation
First-pass effect
Branch of pharmacology concerned with effects of drugs and the mechanism of their action
Pharmacodynamics
Branch of pharmacology concerned with movements of drugs within the body
Pharmacokinetics (ADME)
It is the accumulation of drug because it cannot be excreted by the body
Cumulation
Drugs contraindicated for glaucoma
Diazepam and anticholinergic drugs
Study of damage to fetus during development?
Study of drug dosage?
Teratology - damage
Posology - dosage
Common teratogenic drugs and their effects
- Phenytoin (anti seizure)
- Thalidomide (anti cancer) - shortened limbs
- Tetracycline (antibiotic) - teeth stain (intrinsic), altered bone growth
Amount of drug that reaches the circulatory system after administration
Bioavailability
Drug pH that influence absorption
Drug must be weak acids (pH 6) or weak bases (pH 8) = more lipid soluble
Influences bioavailability
Drug solubility
Route
First-pass effect
dosage of drug needed to produce an effect
potency
refers to the effect of a drug
efficacy
*a drug can be more potent but less efficacious (fentanyl is more potent that morphine)
maximum effect of a drug where no effect is added even though drug dose is increased
maximal effect
a ratio that measures the relative safety of a drug
therapeutic index
TI = LD50/ED50 or TI = TD50/ED50
LD50 - median lethal dose (kill 50% of population)
TD50 - median toxic dose
ED50 - median effective dose (dose that is effective to 50% of population)
higher TI means safer drug
targets of drug action
- receptors
ex. narcotics ➡️ opioid receptors (mu, kappa, delta)
pilocarpine ➡️ muscarinic receptors
epinephrine ➡️ adrenergic receptors - enzymes
ex. MAO inhibitor ➡️ monoamine oxidase
anti-cholinesterase ➡️ acetyl-cholinesterase
ability of drug to bind to its target site
affinity
Ability of drug to procude an effect after binding to its target site
intrinsic activity
*all drugs have affinity but NOT all drugs gave intrinsic activity
full agonist vs antagonist vs partial agonist
FA - elicits maximal response by activating all or a portion of the receptors (ex. Pilocarpine)
antagonist - with affinity but no intrinsic activity (belladona alkaloids - atropine and scopolamine aka hyoscine butylbromide)
partial agonist - with affinity but lesser intrinsic activity; produces less maximal response even all the receptors are occupied (acts as agonist and antagonist)
clark’s occupational theory vs paton’s rate theory
clark - drug effect is proportional to the number of receptors occupied
paton - drug effect is proportional to the rate at which drug and receptor combine
types of sedation
- minimal (conscious) - relieves anxiety
- moderate (depressed consciousness) - can still respond to external stimuli
- deep (depressed consciousness) - only responds to painful and repeated stimuli
Ultra-short acting barbiturates
Methohexital and Thiopental
Short-acting barbiturates
secobarbital and pentobarbital
used for insomnia
intermediate acting barbiturates
amobarbital and butabarbital
used for insomnia
long acting barbiturates
phenobarbital, mephobarbital and primidone
used for induction of general anesthesia
Sedative
**ultra-short acting barbiturates **(thiopental, methohexital)
anticonvulsants/antiseizures
Benzodiazepines (non-barbiturate sedative) ex. Midazolam (most common), diazepam, lorazepam (short-acting)
barbiturates vs non-barbiturates
barbs - more potent, with barbaric acid
non - barbs - less potent, without barbaric acid
common sedative drug used in pediatric patients
Chloral hydrate (non-barbiturates)
non-barbiturate drug that is an anxiolytic but also an antihistamine and anti-cholinergic
diphenhydramine
mechanism of action of sedatives (barbiturates and non-barbiturates)
- affects reticular activating system (RAS)
- activates GABA receptors (gamma amino butyric acid) - inhibition of the different parts of CNS
most common inhibitory neurotransmitter
gamma amino butyric acid
Other inhibitory: glycine, serotonin, dopamine
Sedative-hypnotics drug uses
sedation
induction of G.A.
insomnia
anti-seizure and anti-anxiety
does not produce analgesia
adverse effects of sedatives
drug dependence
stimulates prophyrin production (porphyrism)
respiratory depression - death
coma
drug interaction of sedatives
increases activity of Liver microsomal enzymes (cp450 = faster metabolism)
increase activity of Coumarin-related agents
*precaution to combine with other CNS depressants
drug interaction of sedatives
increases activity of Liver microsomal enzymes (cp450 = faster metabolism)
increase activity of Coumarin-related agents
*precaution to combine with other CNS depressants
common anti-convulsant/anti-seizure drugs
benzodiazepines
phenytoin/ diphenylhydantoin / dilantin
carbamazepine / tegretol
valproic acid
barbiturates
anti seizure drug that is also anti-arrhythmic
phenytoin/ diphenyldantoin / dilantin
anti-seizure drug that is also a treatment of tic douloureux
carbamazepine
mechanism of action of anti-convulsants/anti-seizures
activates GABA receptors
like the sedatives
mechanism of action of anti-convulsants/anti-seizures
activates GABA receptors
like the sedatives
drug uses of anti-seizures
anti-convulsant/anti-seizure or anti-epileptic
anti-anxiety (benzos)
induction of anes (benzos)
insomnia
adverse effects of anti-seizures/anti-epileptic
severe sedation
paradoxical excitement (benzos, nitrous oxide)
drug dependence
respiratory depression
gingival hyperplasia (phenytoin / diphenylhydantoin/ dilantin)
drug interaction: anti-seizures
precaution to combine with other CNS depressants
diazepam is slowly and poorly absorbed in what route of admin?
intramuscular route
drugs with anticholinergic effects but are not generally anticholinergics?? secondary effect lang nila yun
DiTriBeAM
Diphenhydramine
Tricyclic antidepressants
benzodiazepines
antipsychotic agents
meperidine (narcotic)
drug interaction types
- synergistic 1 +1 > 2 (CNS depressants - SNAB)
- additive 1 + 1 = 2 (nsaids and corticosteroids)
- antagonistic 1 + 1 = 0 (narcotic and naloxone)
- potentiation 1 +0 = 2 (paracet and caffeine)
CNS depressants
sedative -hypnotics
narcotics
alcohol
benzodiazepine
Tx for herpes zoster
Aka shingles from VZV
Acyclovir