pharm 2 Flashcards
Oral drugs – undergo
1st pass metabolism in liver.
What is used to determine whether a drug will cross glomerulus: attached to a protein or not;
acid or base; positive or negatively charged
attached to a protein or not
Which drug absorbs better in stomach acid?
Weak acid
In order for a drug to do its effect in what state should it be? Weak acid, Weak base Liposoluble Hydrophobic Hydrophilic
Liposoluble
- NON ionized drugs are soluble in lipid.
When a drug does not exert its maximum effect is because it’s bound to?
Albumin
Which of the following best explains why drugs that are highly ionized tend to be more rapidly excreted than those that are less ionized? The highly ionized are A. less lipid soluble. B. less water soluble. C. more rapidly metabolized. D. more extensively bound to tissue.
A. less lipid soluble.
Therapeutic Index LD/ED is a measure of:
safety of drug
QUESTION: LD50 means at this dose,
50% of the test animals died
QUESTION: What is bioavailability of a drug?
amount of drug that is available in blood
What does bioavailability measured?
How much drug is absorbed in the circulation
Blood to urine ratio
How much drug is absorbed in the circulation
What pharmacokinetic factor influences the need for multiple doses in a day (dose rate)? half-life; bioavailability, or
clearance
half-life
Two different drugs with same dosages, bind to the same receptor, and cause same intrinsic affect. However, they have different
affinities for the receptor. In which aspect these 2 drugs are similar?
a. ED50
b. LD50
c. Potency
d. Efficacy
- Efficacy bc they can both produce the same maximal response if enough is given
Fixed dose drug A w/ low dose of Drug B increase drug B effect when same dose of drug a is give w/ increased does of drug B:
competitive antagonist, synergism, partial agonist
- partial agonists bind & activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist.
Three carpules (2 ml carpules, 40 mg/ml) of local anesthetic X are required to obtain adequate local anesthesia. To obtain the same
degree of anesthesia with local anesthetic Y, five carpules (2 ml carpules, 40 mg/ml) are required. If no other information about the two drugs is
available, then it is accurate to say that drug X:
is less potent than drug Y.
is more efficacious than Y.
is less efficacious than drug Y.
X&Y are = in potency & efficacy.
X is more potent
no info on efficacy really
if ceiling effect was the same but with different doses,
efficacy would be the same
The maximal or "ceiling" effect of a drug is also correctly referred to as the drug's A. agonism. B. potency. C. efficacy. D. specificity.
efficacy
vagal reflex
reflex to suddenly increased BP –> slows down HR
can give atropine to block
Epinephrine reversal –
when also taking α blocker (ex. prazosin, chlorpromazine) cause decrease in BP b/c β-mediated vasodilation
predominates
o Beta2 trumps A1 so vasodilation happens & BP decreases
Alpha-1 agonist:
increase smooth muscle tone, vasoconstrictor –> ↑ BP
Alpha-2 agonist:
given orally b/c they cause hypotension by reducing sympathetic CNS outflow
What does Alpha-1 do?
Vasoconstriction of peripheral vessels (smooth muscle)
When you stimulate alpha 1 receptors what happens?
a. Vasoconstriction
b. Hypertension
Vasoconstriction
What does alpha-1 receptors do to the heart?
Vasoconstriction, increase blood pressure, increase peripheral resistance, mydriasis
(pupil dilution) and urinary retention
Adrenalin – stimulates which receptors
alpha 1, 2 and beta 1, 2 receptors
Heart has which receptors.
beta-1
Slow infusion of epinephrine will cause which of the following and know which receptor is responsible -
Alpha 1 (Vasoconstriction during anaphylaxis), Beta 1 (Increases cardiac output), Beta 2 (bronchodilation)
Patients BP spike after EPI, what receptor?
B1
Hemostatic agents in retraction cord target what receptor? • a1 • b1 • b2 • gaba • muscarinic receptor
a1 (vasoconstriction)
Retraction cord with epinephrine can cause:
increase HR, BP
- do not use in hyperthyroid or cardiac disease.
After using a gingival retraction cord, tissue reacts by recession. Where do you see this the most? Lingual, buccal, interproximal.
buccal
Smooth muscle relaxation is caused by which of the following drugs?
a. prazosin
b. atropine
c. theophylline
d. amphetamine
a. prazosin (alpha 1 blocker…blocks vascular smooth muscle constriction)
b. atropine (anticholinergic)
c. theophylline (treat asthma, COPD…it relaxes bronchial smooth muscle…so I guess it does do smooth muscle…)
d. amphetamine (psychostimulant…increase wakefulness)
- answer should be an alpha-1 antagonist/blocker
Which of the following combinations of agents would be necessary to block the cardiovascular effects produced by the injection of a sympathomimetic drug? Atropine and prazosin Atropine and propranolol Prazosin and propranolol Phenoxybenzamine and curare Amphetamine and propranolol
Prazosin and propranolol
- sympathomimetic drug injection (ex. NE) stimulates α/β receptors so α-blocker prazosin + β blocker propranolol is needed.
- Atropine is an muscarinic/cholinergic receptor blocker that would stimulate heart (opposite effect)
Each of the following drugs produces vasoconstriction of vessels if injected into the gingiva EXCEPT one. Which one is this EXCEPTION? Epinephrine (EpiPen®) Terazosin (Hytrin®) Levonordefrin (Neo-Nedfrin®) Phenylephrine (Neo-Synephrine®) Norepinephrine (Levophed®)
- Terazosin, selective alpha-1 antagonist, is used to tx HTN & enlarged prostate (BPH)
Epinephrine + propanolol:
increases BP, decreases HR
Propranolol is a nonselective beta blocker so epi only acts at only alpha receptors, which in the periphery are mainly alpha-1 receptors
- This causes vasoconstriction &Increased ⬆ BP –> increased firing, which triggers aortic and carotid sinuses –> increased vagal activity
on the heart –> decreased
⬇ HR.
If using with epi, Change propranolol for?
Metoprolol … little change on HR, but no marked increase in BP.
- METOPROLOL = selective B blocker (proprano is nonselective) and is ok to use with EPI!
Propranolol + epinephrine = bad reaction due to: drug interaction, anxiety, allergy
drug interaction,
Patient taking propranolol with epinephrine. What receptor caused hypertensive crisis?
- alpha 1
- alpha 2
- beta 1
- beta 2
alpha-1
- If a patient on a nonselective beta-blocker receives a systemic dose of epinephrine, however, the beta-blocker prevents the
vasodilation, leaving unopposed alpha vasoconstriction. (alpha-1)
What is the effect seen when propranolol and epinephrine are injected simultaneously -
in cases of mild reactions it causes
hypotension; in severe reaction it is malignant hypertension
All these drugs alter ionic movement except - Propranolol, CCB, HCTZ, and Digoxin
Propranolol
QUESTION: A patient receiving propranolol has an acute asthmatic attack while undergoing dental treatment. The most useful agent for management to the condition is? a. Morphine b. Epinephrine c. Phentolamine d. Aminophylline e. Norepinephrine
- Aminophylline: Bronchodilator, class theophylline
The drug-of-choice for the treatment of adrenergically-induced arrhythmias is: quinidine. lidocaine. phenytoin. propranolol
propranolol
Direct alpha sympathomimetic: clonidine, guanethidine , methyldopa
clonidine
guanethidine is indirect - acts on neurons to inhibit NE release
methldopa is fake neurotransmitter
Epinephrine Reversal with?
Alpha adrenoceptor blockers (ex. phenoxybenzamine)
- inhibit the vasoconstrictor effect but not the vasodilator effect of epinephrine = low BP instead of high BP
Epinephrine reversal: after giving a patient epinephrine, following hypertension, which of these drugs would cause a drop in BP?
Phenoxybenzamine
What receptor or signaling pathway is linked most directly to α2-adrenoceptor stimulation? I
nhibition of adenylyl cyclase through
GI, resulting from stimulation of α2-adrenergic receptor, leads to intracellular ⬇ cAMP
amphetamines MOA
indirect-acting sympathomimetics
ADHD meds
Methylphenidate = Ritalin
o Methylphenidate: blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins.
- Amphetamine = Adderall
o Amphetamines & cocaine: increase catecholamine NE SERETONIN DOPAMINE release as a primary mechanism.
§ Amphetamines stimulate CNS alpha receptors
o Adderall: psychostimulant medication composed of amphetamine and dextroamphetamine, which increases the amount of
dopamine and norepinephrine in the brain
ADHD with gender
M>F
Amphetamines MOA –
lead to NE release in brain
- stimulate the release of norepinephrine from central adrenergic receptors & at higher dosage, release of dopamine
Methylphenidate brand name, Amphetamine brand name
Methylphenidate = Ritalin, Amphetamine = Adderall.
Kid is taking Adderall (amphetamine) & is very anxious what do you do?
Tell him to stop taking amphetamine on the day
appointment
- Amphetamine can induce anxiety, and are contraindicated for patients that are very nervous
Side effect of Amphetamines
– Insomnia (difficulty of falling asleep)
Amphetamines, what are symptoms?
Increased heart rate & excitability
Cholinergic crisis:
bradycardia, lacrimation, salivation, voluntary muscle weakness, diarrhea, bronchoconstriction – tx w/ atropine
cholinergic agonists: examples and effect on slivation
increased salivation
pilocarpine (direct), neostigmine
anticholinergic agents
atropine/scopolamine
antticholinergic overdose
confusion, hallucinations, burning mouth, hyperthermia – tx w/ physostigmine
direct cholinergic agonist
pilocarpine, methacholine (xerostomia)
indirect acting cholinergic agonists MOA
prevent enzyme breakdown
reversible anti-cholinesterase: physostigmine (CNS and PNS) and neostigmine (PNS only)
irreversible = insecticides and organophosphates
tx overdose with pralidoxime
Competitive muscarinic receptor blockers =
Atropine, scopolamine, propantheline
What is used for motion sickness?
scopolamine
Neostigmine and pilocarpine increase?
Salivation
- Pilocarpine (muscarinic agonist) & neostigmine are parasympathomimetic that acts as a reversible acetylcholinesterase inhibitor. They
increase salivation, urination, bronchoconstriction, bradycardia, miosis (pupil constrict), vasodilation
Glycopyrrolate effect?
reduce salivary (muscarinic anticholinergic)
Atropine: _____ salivation
decrease
What meds decrease saliva?
atropine, scopolamine
- Pilocarpine, methacholine, neostigmine, etc. cause salivation.
QUESTION: If patient has xerostomia, what medication won’t you give?
Atropine - anticholinergic
What drug does not cause miosis of the eyes?
Atropine
Pt have bradycardia, what should we give him?
Atropine b/c atropine will increase heartrate causing tachycardia.
Drug to decrease saliva because you want to take an impression- Atropine, Pilocarpine, Neostigmine
ATROPINE
Atropine poisoning tx:
physostigmine
Patient salivates a lot, what is tx before surgery?
Atropine **antimuscarinic
Xerostomic pt, give
pilocarpaine or cevimeline.
- Cimeviline just like pilocarpine to increase salivation in xerostomia
What drug do you give to a pt with xerostomia?
Pilocarpine
Pilocarpine used for?
parasympathomimetic alkaloid, for tx of glaucoma and xerostomia.
What is the side effect of pilocarpine (Tx of dry mouth) in toxic dose?
Bradycardia and hypotension
Apnea
Cardiac shock
Bradycardia and hypotension
- nontoxic side effects»> excess sweating and salivation, bronchospasm
Propantheline bromide (pro-Banthine):
anti-cholinergic (anti-muscarinic), relieve cramps or spasms of the stomach, intestines, and
bladder.
Which of the following groups of drugs is contraindicated for patients who have glaucoma? Adrenergic, Cholinergic, Anticholinergic
Adrenergic blocking
Anticholinergic
Which of the following drug groups increases intraocular pressure and is, therefore, contraindicated in patients with glaucoma? A. Catecholamines B. Belladonna alkaloids C. Anticholinesterases D. Organophosphates
B. Belladonna alkaloids – anti-cholinergic
organophosphates are irreversible cholinesterase inhibitors; indirect agonists
tubocurarine
inhibits ACH receptor –> weakness of skeletal muscles
Decrease of pseudocholinesterase would lead to increase in? Succinylcholine or tubocurare
Succinylcholine
Administration of succinylcholine to patient deficient in serum cholinesterase would cause…
a. convulsions
b. Hypertension
c. prolonged apnea
d. Acute asthma attack
c. prolonged apnea
miosis can be caused by which drigs
opioids and cholinergics
mydriasis can be caused by which drugs
anticholinergics and increased serotonin
A patient who has Parkinson’s disease is being treated with levodopa. Which of the following characterizes this drug’s central
mechanism of action?
a. it replenishes a deficiency of dopamine
b. it increases concentrations of norepinephrine
c. it stimulates specific L-dopa receptors
d. it acts through a direct serotonergic action
a. it replenishes a deficiency of dopamine
Cause of Parkinson?
Dopamine deficiency, give them methyldopa (levodopa) to increase dopamine in the CNS
Why do you need to take carbidopa with levodopa:
prevents breakdown of levodopa before it crosses the blood brain barrier
Carbidopa addition prevents levodopa from being converted into
dopamine in the bloodstream, peripheral enzymatic degradation so more reaches the brain.
How does carbidopa tx Parkinson’s disease?
potentiates effects of dopamine
anti-psychotics effect
sedate, blunt emotional expression, attenuate aggressive & impulsive behavior.
anti-psychotics adverse effects
Produce anticholinergic adverse effects,
dystonias and extrapyramidal symptoms. Tardive dyskinesia most common after several years.
tardive dyskinesia whose side effect
anti-psychotics
phenothiazine
Phenothiazines (PTZ) MOA :
Block DA receptors, act on the extrapyramidal pathway
Where in the brain does anti-psychotics works?
blocking the absorption of dopamine
extrapyramidal pathways
What catecholamine does Phenothiazine (anti-psychotic) affect? Dopamine, serotonin, acetylcholine
Dopamine
Phenothiazine side effect:
Tardive Dyskinesia
proverbial anti-psychotic
phenothiazine
What acts on extrapyramidal?
Phenothiazines (chlorpromazine)
Onset of action of antipsychotic is:
5-6 days
Lithium is used for treatment of?
Manic phase of bipolar disorder
Patient is in her 70’s, she lives alone, what could she be suffering from?
Depression
Most common psychological problem in elderly?
Depression
Old people have dementia as the most prominent psychiatric issue:
depression
What is associated with depression? Age, economic status, professional status, etc
Age
Most common mental illness among elderly?
Depression
Main sign of dementia: a. confusion b. short term memory loss c. long term memory loss -
b. short term memory loss
short term memory loss = first main sign. Long term loss occurs later.
Where in the brain does anti-depressants works?
decrease amine-mediated neurotransmission in the brain
Tricyclic anti-depressant (TCA) mechanism of action:
inhibit reuptake of NE and 5-HT (serotonin)
TCA 2nd generation-
-triptylines and -pramines
How do tricyclics work?- by
not allowing reuptake of neurotransmitter (NE, 5-HT, serotonin)
What catecholamine do tricyclic antidepressants affect? Dopamine, serotonin, acetylcholine
serotonin
Patient is taking TCA anti-depressants what do you take into consideration? Limit duration of procedures, keep in mind the
epinephrine limit
keep in mind the
epinephrine limit
Side effect of having TCA and epi: HTN, hypotension, hyperglycemia, hypoglycemia
HTN
Most common antidepressant does what?
- Inhibits reuptake of NE, 5-HT, & DA (TCA)
- Inhibit reuptake of 5-HT (SSRI)
- Inhibit reuptake of N & 5-HT (SNRI)
- Inhibit MAO; prevent breakdown of NE & 5-HT (MAOI)
- Block D2 receptor (phenothiazine)
If someone has a history of depression & wants to quit smoking, what do you give?
Zyban (Bupropion), it’s an anti-depressant &
smoking cessation aid
- not Chantix (smoke cessation only)
Amitriptyline –
most common tricyclic antidepressant, inhibits reuptake of NE and serotonin
Zoloft works on what receptor?
Presynaptic monoamine transporters (inhibit reuptake of 5-ht)
- Sertraline hydrochloride (Zoloft) = selective serotonin reuptake inhibitor (SSRI)
Prozac (fluoxetine) -
acts on serotonin (SSRI)
What do you use St. John’s Wart?
Depression
- St. John’s Wart = noncompetitive reuptake inhibitor of serotonin yeah because is for depression
What does St. John’s Wart do (side effect)?
Decrease the body immunity
St johns wart- used for?
Depression, don’t use with benz and HIV medication
- In HIV pt, it interacts w/ anti-HIV drugs & reduces their function so the immunity decreases
Know drugs used for conscious sedation à
SSRIs/BDZ Diazepam and Prozac (fluoexitine)
Buspirone -
psychotropic w. anxiolytic; low CNS depression, low psychomotor skill impairment
- Buspar—different from benzodiazepines because it does NOT cause CNS depression, muscle relaxant, or anti-convulsant!!!!!** UNIQUE!!!
Anxiolytic and antidepressant
side effect of corticosteroids
gastric ulcers, immunosuppression, acute adrenal insufficiency, osteoporosis, hyperglycemia, redistribution of body fat.
Strongest glucocorticoid/long-acting Corticosteroid?
Dexamethasone
Negative effect of chronic use glucocorticoids? In
fection, reduce inflammation, hyperglycemia.
GI effects with corticosteroids: .
Ulcers
Long term side effect of corticosteroids-
osteoporosis and hyperglycemia
What is the side effect of prolonged corticosteroid therapy?
Osteoporosis
Too much cortisone causes what to bone?
Osteoporosis
Osteopetrosis
Osteosclerosis
Osteoporosis
Where do you see moon faces?
steroid treatment
Containdation for corticosteroid use:
diabetes (also: HIV, TUBERCULOSIS, CADIDIASIS, PEPTIC ULCER)
Aspirin contraindicated with:
corticosteroid use
Critical dose of steroids for adrenal insufficiencies -
20 mg of cortisone or its equivalent daily, for 2 weeks within 2 years of dental
treatment
QUESTION: Least amount of cortisone to affect the adrenergic system?
2 mg for 2 weeks for 2 years
Pt taking corticosteroid with rheumatoid arthritis, pt needs TE, why would you consult with physician?
full blood panel, assess for
adrenal insufficiency
- want to make sure pt can produce enough corticosteroid with addition to what they are taking so you won’t have over inflammatory
response from TE
Pt on 3 months tx of steroids, what is your tx?
no tx and consult GP for dose
If a pt. has been using 10 mg of corticosteroid for 10 years, what would you do for pt. before any tx?
Have pt continue and increase
the dose
Cortisone exerts its action by binding to intracellular receptor, receptors on membrane, proteins in plasma
intracellular receptor
- Enter cell and bind to cytosolic receptor migrate to nucleus gene expression or with plasma membrane on target cells
QUESTION: If pt doesn’t get steroid tx in time for their temporal vasculitis, what will have happened?
• hearing loss
• vision loss
• retro-ocular headache
• vision loss
Asthma – long-term asthma give corticosteroid to
decrease inflammation
- Inhaled corticosteroids are the most effective medications to reduce airway inflammation and mucus production.
absolute contraindication for nitrous oxide
severe respiratory compromised, COPD, respiratory infection, pneumothorax/collapsed lung
relative contraindications for nitrous
cardiovascular conditions, pregnancy (teratogenic effect), nasal congestion, children with high anxiety,
Nitrous oxide is in which container
blue cylinder (oxygen in green)
Nitrous oxide MOA
oxidizes the cobalt in vitamin B12, resulting in the inhibition of methionine synthase. Nitrous oxide has greater
analgesic potency than other inhaled anesthetics
Dreaming while on nitrous is what? Overdose or normal
normal