Pharmacology 4 Flashcards
Name 4 therapeutic effects of aspirin.
Pain relief
Antipyretic effects
Antirheumatic effects
Anti-inflammatory effects
Adverse or toxic effects of aspirin include what 9 things?
Occult bleeding from GI tract
Tinnitus
Nausea and vomiting
Acid-base disturbance of metabolic acidosis
Decreased tubular reabsorption of uric acid
Salicylism
Delirium
Hyperventilation
Acetaminophen lacks ___ activity. It is hepatotoxic and [causes/does not cause] GI upset
Anti-inflammation
Does not cause
Which causes more GI irritation, ibuprofen or aspirin?
Aspirin
True or false… diflunisal (dolobid) has a longer half-life than aspirin, acetaminophen, and ibuprofen
True
Acetaminophen causes liver toxicity, especially when combined with __ or taken in excess of ___ per day.
Alcohol
4grams per day
____ is the drug of choice for the feverish child? Why should aspirin be avoided?
Acetaminophen
Increased risk of Reye’s syndrome
The mechanism of the antipyretic action of salicylates probably results from…
Inhibition of prostaglandin synthesis in the CNS affecting hypothalamic temperature regulation
True or false.. the antipyretic action of salicylates is explained in part by cutaneous vasoconstriction leading to increased heat loss
False.. cutaneous vasoDILATION leading to increased heat loss
___ is the locus of action of aspirin’s central antipyretic effect
Hypothalamus
A patient who has been taking large quantities of aspirin might show increased postoperative bleeding because aspirin inhibits…
Synthesis of thromboxane A2 and prevents platelet aggregation
True or false… triamcinolone directly inhibits prostaglandin synthetase
False… it inhibits phospholipase A2, the enzymatic step that precedes prostaglandin synthesis. Triamcinolone is a corticosteroid, this is how corticosteroids work.
True or false… phenylbutazone is an NSAID
True
Which of the following is NOT produced by excessive doses of acetylsalicylic acid?
Delirium Tinnitus Hypothermia Hyperventilation Metabolic acidosis
Hypothermia - it only lowers your temperature if you have a fever. Taking aspirin does not have any affect on body temperature in the non-feverish patient, but high doses can cause all the other effects listed.
True or false… acetylsalicylic acid causes methemoglobinemia
False
True or false… aspirin causes decreased tubular reabsorption of uric acid
True
True or false… acetaminophen may cause methemoglobinemia at high doses
True
True or false… acetaminophen is cross-allergic with aspirin.
False
___ is used in detoxification of opioid addicts
Methadone
Name 7 pharmacological effects of morphine
Respiratory depression
Euphoria
Sedation
Dysphoria
Analgesia
Constipation
Urinary retention
What is the mechanism of respiratory depression in an opioid overdose?
Loss of sensitivity of the medullary respiratory center to carbon dioxide
True or false… narcotic ingestion can lead to bronchiolar constriction and increase in intracranial pressure
True
Which drugs suppress the cough reflex?
Opioids
Morphine binds to ___ receptors in the __ to produce analgesia
Mu
CNS
Morphine causes vomiting by…
Stimulation of the medullary chemoreceptors trigger zone
Barbiturates and opiates depress respiration primarily by…
Rendering the respiratory center in the brain stem less sensitive to changes in CO2
The cause of death with opioid intoxication is ___
Respiratory depression
True or false… pentazocine has both agonistic and antagonistic activities
True
A heroin-dependent patient should NOT be given nalbuphine for pain because…
As a mixed agonist-antagonist, it can elicit withdrawal symptoms
True or false… pentazocine is effective only on parenteral administration
False.
Why is methadone used in detoxification (drug withdrawal) of patients physically dependent on morphine?
Withdrawal reactions are less intense and stressful than those of morphine
True or false… methadone is a full agonist with analgesic properties, just like morphine
True. However, when taken orally, it is not euphoric in addicts, but acts just like morphine to produce tolerance and physical dependence. Withdrawal is less severe than with morphine because methadone has a much longer Half life.
___, ___, ___ are competitive muscarinic receptors blockers which sometimes are used to control salivary secretions. ____ specifically, blocks vagal reflexive control of heart rate, resulting in tachycardia
Atropine
Scopolamine
Propantheline
Atropine
___ and ___ are reversible anticholinesterase that differ in that ___ acts both centrally and peripherally whereas __ only acts peripherally but also has some direct ACh-like activity at the neuromuscular junction, in addition to prolonging the activity of endogenous ACh. They sometimes see use in treating xerostomia
Physostigmine
Neostigmine
Physostigmine
Neostigmine
___ and ___ are direct acting cholinergic agonists. They may be used for xerostomia
Pilocarpine
Methacholine
Organophosphates and incentivized irreversibly inhibit ___
Cholinesterase
___ is an enzyme regenerator used in organophosphate toxicity
Pralidoxime
___ is a depolarizing neuromuscular junction blocker, subject to rapid inactivation by plasma pseudocholinesterase. It is used to prevent laryngospasm
Succinylcholine
___ is a non-depolarizing neuromuscular junciton blocker
D-tubocurarine
__ and ___ are ganglionic blockers that produce orthostatic hypotension
Mecamylamine
Hexamethonium
Name 6 symptoms of a cholinergic crisis. What do you use to treat it?
Bradycardia Lacrimation Salivation Voluntary muscle weakness Diarrhea Bronchoconstriction
Atropine
What are 5 symptoms of a scopolamine overdose? What do you use to treat it?
Disorientation Confusion Hallucinations Burning dry mouth Hyperthermia
Physostigmine
Atropine blocks the __ reflexive control of heart rate, resulting in [bradycardia/tachycardia]
Vagal
Tachycardia
Neostigmine produces its effect by ___
Inhibition of acetylcholinesterase activity (similar to physostigmine, however these differe from the insecticides and nerve gases listed below in that they are reversible and can be used clinically; the latter are irreversible)
Name two ganglionic nicotinic blocking agents
Mecamylamine
Trimethaphan
How can neostigmine stimulate denervated skeletal muscle?
It is capable of acting directly on the endplate
Which drug can be used to prevent laryngospasm?
Succinylcholine (it is a nicotinic antagonist - skeletal muscle relaxant)
Outline the cholinergic stimulation effects
Eye: miosis and reduction of intraocular pressure
CV: bradycardia; vasodilation (but only from injected cholinergic agents, since the muscrinic receptors on the vascular smooth muscle has no neural input)
GI tract: increased spasmodic activity, increased salivation and acid secretion (overdose; nausea, vomiting, diarrhea)
urinary tract: increased uringation
Resipiratory: bronchoconstriction
Glandular: lacrimation, sweating
Skeletal muscle: tremor and ataxia (overdose; muscle weakness, cramps and fasiculations)
out line the anticholinergic (antimuscarnic) actions
Eye: mydriasis and loss of accommodation and increase of intraocular pressure
CV: increased heart rate (overdose: tachycardia
GI tract: decreased spasmodic activity, decreased salivation and acid secretion (overdose)
Urinary tract: decreased urination
Respiratory: bronchodilator
Glandular: decreased lacrimation, decrease sweating (overdose: hot, dry skin, hyperthermia)
Skeletal muscle: no effects, since they don’t act on nicotinic receptors, only muscarinic
CNS: tertiary amines such as atropine get into the brain and cause restlessness, headache, excitement, hallucinations and delirium
Quaternary amines like methantheline and propantheline only have peripheral actions
How does tachycardia result from administration of atropine or scopolamine?
Blockade of vagus nerve activity
Atropine and scopolamine are muscarinic cholinergic receptor blockers.
All of the following are possible effects of cholinomimetic drugs except…
Mydriasis Bradycardia Increased peristalsis Stimulation of sweat glands Increased secretion by bronchial glands
Mydriasis
True or false.. in addition to anticholinergic effects, atropine overdose causes CNS excitation and tachycardia
True
This is atropine isn’t used for sedation. (Scolopamine may be used for sedation because it doesn’t have this effect)
True or false physostigmine is an indirect acetylchoniesterase that will function to increase cholinergic action
True
Succinylcholine is a short-acting neuromuscular junction blocking agent useful for providing a brief paralysis to aid in incubating patients. It is short-acting because…
It is subject to inactivation by plasma esterases
Receptor blockers (alpha or beta adrenergic drugs such as prazosin or propranolol respectively) act by [competitive/noncompetitive] inhibition of ____ receptors
Competitive
Postjuncitonal
What is reserpine?
Depletes NE by inhibiting its reuptake
What is guanethidine?
Inhibits the release of catecholamines
What is alpha methyldopa?
Acts centrally as a false neurotransmitter which gets taken up into storage vesicles and released with NE, thus decreasing sympathetic activity
What is clonidine?
Stimulates A2 receptors in CNS with a resulting decrease in sympathetic outflow
What is “epinephrine reversal”?
In the presence of an alpha blocker (usually they give prazosin, but drugs such as chlorpromazine may also be given) epi causes decrease in blood pressure rather than increase because beta mediated vasodilation predominates
What is the vagal reflex?
Injection of a pressor dose of NE may result in decreased heart rate due to activation of barorecptors which stimulate vagal reflex to reduce heart rate.
The vagal reflex is blocked by which drug?
Atropine
What are the results of alpha-1 receptor stimulation? (3 things)
Vasoconstriction
Urinary retention
Mydriasis
Name three effects of beta receptor stimulation.
Increased heart rate (b1)
Bronchodilation (B2)
Vasodilation (B2)
Alpha-1 block results in vaso[dilation/constriction].
Vasodilation
What happens when beta receptors are blocked?
Decreased heart rate (B1)
Bronchoconstriction (B2)
Carbidopa is given with levodopa to block ___ activity in the periphery, which in the absence of carbidopa, converts the levodopa to DA in the periophary, decreasing the amount of levodopa that ends up in the brain. ___ is sympathomimetic, and will produce sympathetic stimulation in the periphery. Results in Development of abnormal facial movement, nausea and vomiting, cardiac arrhythmias, and mental disturbances.
Dopa decarboxylase
Levodopa
Describe the mechanism of action of guanethidine
Uncoupling of the action potential from the NE release mechanism
___ and ___ are the only centrally acting antihypertensives, reducing sympathetic outflow via alpha-1 agonist action.
Methyldopa
Clonidine
What is the mechanism of action of reserpine?
Stabilize the axon terminal membrane thus preventing release of NE
Pretreatment with ___ prevents a response to amphetamines because…
Reserpine
Causes depletion of NE from storage sites, thus it cannot be released by amphetamine.
What are the effects of alpha 1 agonists?
Increased smooth muscle tone leading to VASOCONSTRICTION and INCREASED blood pressure
What are the effects of alpha-2 agonists?
Can cause hypotension by reducing sympathetic outflow from the CNS
What are the affects of B-1 agonists?
Increased cardiac rate and force of contraction, thus positive inotropic and chronotropic actions
What are the effects of Beta-2 agonists?
Dilation of skeletal muscle blood vessels and bronchi or relaxation of bronchiolar smooth muscle
Phenolamine is a ___ blocker.
Alpha
Injection of epi usually causes a rise in blood pressure due to what 3 things?
Myocardial stimulation that increases ventricular contraction
An increase in heart rate
Vasoconstriction due to alpha receptor stimulation
True or false… NE stimulates alpha and beta 1 receptors more than beta 2
True
Phenylephrine is a ___ agonist used for ___
Alpha-1
Stuffy noses
___ is the phenomenon in which two drugs produce opposite effects on a physiologic system but do not act at the same receptor site.
Physiologic antagonism
_____ reactions to drugs are related to genetic factors and they are the least predictable.
Idiosyncratic
Two drugs, A and B, have the same mechanism of action. Drug A in a dose of 5mg produces the same magnitude of response as drug B in a dose of 500mg. Drug A is 100x as ___
Potent
What is the occupational theory of drug-receptor interaction?
The magnitude of the drug response is proportional to the number of receptors occupied
An antagonist drug has affinity but no intrinsic activity
The degree of drug action is dependent on the law of mass action
What is the mechanism of action of benzodiazepines?
Modulate the activity of the inhibitory neurotransmitter, GABA
What are 4 advantages of benzodiazepines over barbiturates?
Less addiction potential
Less profound CNS depression
Larger therapeutic index
Less respiratory depression
IV injection of diazepam can cause irritation such as ____ due to solvent in the benzodiazepine is dissolved in.
Thrombophlebitis
Also note that many benzos form active metabolites
Thiopental’s action is terminated by…
Redistribution of the drug out of the brain. It enters the brain rapidly and exits rapidly. Thus it has a quick onset and short duration of action
True or false… barbiturates provide profound analgesia
False.. barbs are not analgesic at all
How are barbiturate overdoses lethal?
Respiratory depression
Barbiturates are contraindicated in pateints with ____ because…
Intermittent porphyria
Barbs enhance porphyrin synthesis and thus will aggravate the disease.
Benzodiazepines exert their main effect on ____
Central GABAergic neurons
Barbiturates [increase/decrease] secretions
Decrease
The action of the ultrashort-acting barbiturates is terminated primarily by the process of ___
Redistribution
Barbiturates are metabolized by the ___, the are classified according to duration of action (thiopental is __acting, phenobarbital is ___acting), and they depress all levels of the CNS
Liver
Thiopental
Phenobarbital
If diazepam is to be given intravenously, it is recommended that a [small/large] vein be used in order to decrease the risk of ___
Large
Thrombophlebitis
What is the mechanism of antipsychotic action?
Blockade of dopaminergic sites in the brain
What are the Two major side effects of antipsychotics?
Anticholinergic effects
Extrapyramidal stimulation resulting in tardive dyskinesia
2nd generation antipsychotics, like clozapine, block __ and ___ receptors. They treat ___ symptoms. They have [fewer/more] extrapyramidal side effects like tardive dyskinesia.
Dopamine
Serotonin (5-HT)
Negative
Fewer
What are the main side effects of antidepressants?
Anticholinergic or atropine-like side effects
___ is the drug of choic for the manic phase of manic depression (bipolar)
Lithium
True or false… antipsychotic drugs cause emesis (vomiting).
False. They are effective ANTIemetics and are often used clinically for this purpose.
Antipsychotics [block/stimulate] the dopamine receptor. They also affect the hypothalamic temperature regulation system
Block
The antipsychotic effects of phenothiazines are the result of ___
Blockade of dopaminergic sites in the brain
___ is the prototypic phenothiazine, an antipsychotic drug used in the treatment of schizophrenia. Other antipsychotic drugs used for this purpose are __ and ___.
Haloperidol
Thioridazine
What is an irreversible side-effect resulting from long-term administration of phenothiazines?
Tardive dyskinesia
Tardive dyskinesia is a neurological side-effect of which drug class?
Phenothiazine antipsychotics
True or false… Phenothiazine derivatives result in gingival hyperplasia
False..
It does result in jaundice, xerostomia, postural hypotension, and symptoms of Parkinsonism
Imipramine is a ___. Tranylcyopromine is a ___
Tricyclic antidepressant
MAOI
What is the major mechanism of action of tricyclic antidepressants?
Blockade of the reuptake of amine neurotransmitters released into the synaptic cleft.
Tricyclic antidepressants have a prominent side effect that most nearly resembles the usual pharmacological action of ___
Atropine
TCAs are strong anticholinergics
True or false… corticosteroids or glucocorticoids suppress the immune system in addition to their antiinflammatory action. This can cause latent TB infections to go systemic
True
Name 8 side effects of corticosteroids/glucocorticoids
Gastric ulcers
Immunosuppression
Acute adrenal insufficiency
Osteoporosis
Hyperglycemia
Redistribution of body fat
True or false… adrenal corticosteroids cause retention of sodium and fluid. They decrease activity in lymphoid tissue. They can produce a diabetes-like syndrome with high blood levels.
True
___ is contraindicated in a patient with AIDS, candidiasis, TB, or peptic ulcers.
Corticosteroids
Glucocorticosteroids are useful as secondary treatment of anaphylaxis because they…
Suppress the inflammatory response to cell injury
___ are used successfully to treat Addison disease, lupus erythematosus, rheumatoid arthritis, and apthous stomatitis.
Adrenal steroids
True or false… the onset of anesthesia is inversely proportional to solubility of the anesthetic in the blood.
True. The more soluble the agent is in the blood, the more must be given to reach critical tension in the brain
The general anesthetic, Halothane, is associated with what adverse side effect?
Hepatotoxicity
Name the 4 stages of anesthesia
Stage 1: analgesia
Stage 2: delirium
Stage 3: surgical anesthesia
Stage 4: medullary paralysis
Signs and stages of anesthesia are most likely to be seen with a general anesthetic that has a [slow/fast] rate of induction
Slow
The behavior of pateints under general anesthesia suggests that the most resistant part of the CNS is the ___
Medulla oblongata
In general anesthesia, the last part of the CNS to be depressed is the __
Medulla (stage 4)
H1 antihistamines are useful for treating ____
Dermatological manifestations of an allergic response (chlorpheniramine)
H1 antihistamines are used preoperatively for ___, ___ properties, and ____ effects.
Sedation
Antiemetic
Anticholinergic
True or false… antihistamines are used in controlling symptoms of Parkinsonism
True (ex. Diphenhydramine)
H2 antihistamines such as cimetidine are used to ____
Reduce gastric acid secretion (now available OTC for heartburn)
What is chlorpheniramine and what is it used for?
Antihistamine (H1)
Used for treating dermatological manifestations of an allergic response
What is cimetidine and what is it used for?
H2 antihistamine. Used to decrease gastric acid secretion
Which antihistamine is most commonly used as preoperative medication?
Promethazine (used for vertigo)
The use of diphenhydramine (Benadryl) in controlling the symptoms of Parkinsonism is based on its ___ effects.
Anticholinergic
The mechanism of action of H1 antihistamines is ___
Competitive antagonism
Which drug is used to treat trigeminal neuralgia?
Carbamazepine
