Pharma Credit II Flashcards
Cocaine produces vasoconstriction because it:
Prevents reuptake of noradrenaline
List the most common prescription medications with potential for interactions with herbal therapy
- Antidiabetics
- Antidepressants
- Anticoagulants
- Analgesics
List the clinical uses and effects of urea:
- Urea is used to treat dry/rough skin conditions
- Hydrating agent for skin
- Used in scaling conditions (psoriasis, eczema)
- Enhances penetration of other topical drugs
Succinylcholine is a:
Depolarising NM blocker
Severe Benzodiazepine overdose can be reversed with:
Flumazenil
Gross structural defects of a foetus can be caused by teratogen in:
First trimester
Give an example of a “time related (delayed) adverse effect”:
— Type D AE: e.g. teratogenic effect of thalidomide→phocomelia — malformations of limbs / Amelia = total absence
— Diethylstilbestrol→induces vaginal cancer in daughters of mothers taking it during pregnancy
— Ethanol→fetal alcohol syndrome
Neuropathic pain – description, basic characteristics, treatment:
Neuropathic pain: pain caused by abnormal neural activity that arises secondary to injury, disease, or dysfunction of the nervous system
Central pain: caused by CNS dysfunction (e.g., from lesions produced by an ischemic stroke, phantom limb pain)
Peripheral pain: caused by damage to peripheral nerves (e.g., diabetic neuropathy, postherpetic neuralgia)
- Pain, paraesthesia and hyperesthesia affecting the somatosensory NS
- 1st line treatment: tricyclic antidepressants (amitriptyline), SNRI (duloxetine), antiepileptics
(pregabalin & gabapentin), 5% lidocaine patches - 2nd line: opioids (tramadol), capsaicin cream (chilli)
What is the effect of
Alpha1 agonists on blood pressure:
Increases blood pressure
The effect of non-depolarizing NM blockers:
— is not competitive
— is reversed by an acetylcholine esterase inhibitor
— is potentiated by an acetylcholine esterase inhibitor
- Is reversed by Ach esterase inhibitors
Clinical use of barbiturates
- Effects are: sedation & CNS depression
- Uses in insomnia & anxiety (pentobarbital), general anesthesia and status epilepticus
(thiopental) and as general anticonvulsant drug (phenobarbital)
Phytotherapy is:
- Safe because natural
- An ineffective placebo
- A useful therapeutic alternative
(- Safe because natural)
(- An ineffective placebo)
- A useful therapeutic alternative — correct
Explain type A adverse drug reaction and give examples:
- Dose dependant adverse reaction
- Common, predictable, low mortality
- Can be managed by reducing dose
- Examples: hypotension caused by antihypertensives, dehydration caused by diuretics,
immunodeficiency and tendency for infections caused by immunosuppressant (cyclosporin A, methotrexate, glucocorticoids)
Potentiation means:
One drug increases the effect of another drug without having the same effect (1+ 0 > 1)
The following effect of adrenaline can be blocked by beta 1 adrenoceptor blockers.
- Constriction of blood vessels
- Dilation of blood vessels
- Increased heart rate
- Increased force of contraction
- Increased systolic blood pressure
Correct are:
- Increased heart rate
- Increased force of contraction
Isoprenaline stimulates:
- Beta 1 and beta 2 receptors
- Selectively beta 2 receptors
- M receptors
- Selectively beta 1 receptors
Correct is:
- Beta 1 and beta 2 receptors
What are emollients?
- Emollients help to keep the skin moist by covering it and thereby reducing water loss
Which of the following statements about neuropathic pain is true ?
- Neuropathic pain responds well to conventional non-opioid analgesics
- Neuropathic pain is usually chronic
- Treatment of neuropathic pain is successful in most patients
Correct is:
- Neuropathic pain is usually chronic
Which pharmacokinetic parameter best describes the absorption of a drug ?
- AUC and maximum concentration (Cmax)
- Clearance and volume of distribution
- Elimination rate constant (ke) and elimination half-life (t1/2)
Correct is:
- AUC and maximum concentration (Cmax)
Succinylcholine:
- Is a long acting NM blocker
- Its effect can be reversed by Ach esterase inhibitors
- Is a depolarizing NM blocker
- Can cause initial fasciculations
Correct is:
- Is a depolarizing NM blocker
- Can cause initial fasciculations
Tubocurarine:
- Acts on muscarinic receptors
- Is a depolarizing NM blocker
- Its effects can be reversed by Ach esterase inhibitors
- Can cause initial fasciculations
Correct is:
- Its effects can be reversed by Ach esterase inhibitors
Common herbs (that are frequently used in phytotherapy) with a high potential for interactions with prescription medications are (two examples):
- St. John’s wort (Serotonin syndrome)
- Feverfew (potentiates platelet aggregation)
- Garlic (potentiated hyperglycaemic and antiplatelet drugs)
- Ginger & gingko (may inhibit platelet aggregation)
- Ginseng (may increase digoxin levels)
- Goldenseal (may oppose anticoagulants)
Explain type B of adverse drug reactions:
- “bizzare”, non-dose related adverse reaction
- Unpredictable, uncommon, high mortality
- Not related to pharmacological action of the drug
- Can be immunological (hypersensitivity) or idiosyncratic (genetically defined)
Drugs used to decrease craving for alcohol are:
- Benzodiazepines, naltrexone, acamprosate
- Naltrexone, tiapridal, acamprosate
- Atenolol, tiapridal, acamprosate
Correct is:
- Naltrexone, tiapridal, acamprosate
Topical corticoids: use and side effects:
- Use: eczema, contact dermatitis
- Side effects: skin irritation, skin thinning, skin infections, allergy to topical drug, systemic side
effects (Cushing’s sy.)
Give at least two examples of drugs that are known to be teratogenic in humans:
- Warfarin→bone defects & internal bleeding→abortion and stillbirth
- Retinoids→facial and cardiovascular abnormalities
- Cytotoxic drugs (e.g. antifolates like methotrexate→neural tube defects)
- Diethylstilbestrol → vaginal carcinoma
- Thalidomide → phocomelia
- Ethanol→fetal alcohol syndrome
- Smoking
The extent of the drug absorption / exporuse is best characterized by:
- The area under the concentration- time curve (AUC)
The specific antidote of opioid analgesics is:
Naloxone
Atropine will oppose the effect of:
Ach on the intestinal smooth muscle
Which of the following drugs are NOT commonly used in psoriasis
- Emollients
- Topical antivirals
- Vit D analogs
Correct is:
- Topical antivirals
Medical plants:
- By definition cannot interact with conventional drugs
- Are safe because natural
- May contain pharmaceutically active substances with both beneficial and harmful effect on
the human body
Correct is:
- May contain pharmaceutically active substances with both beneficial and harmful effect on
the human body
Which of the following drugs are relatively safe during pregnancy?
- Telmisartan (an antagonist of angiotensin receptor)
- Folic acid
- Tetracycline
Correct is:
- Folic acid
Some drugs are effective in the treatment of neuropathic pain when administered locally, e.g.:
- Duloxetine
- Carbamazepine
- Capsaicin
Correct is:
— Capsaicin
Sympathetic autonomous nevres:
— cause the release of noradrenaline and activation of beta 1 adregenergic receptors in the heart
— release noradrenaline in preganglionic neurons
— Have positive inotropic effect on the heart through activation of beta 1 adrenergic receptors
Have positive inotropic effect on the heart through activation of beta 1 adrenergic receptors
Muscarinic receptor antagonists will:
- Increase heart rate
- Slow down heart rate
- cause bronchoconstriction
Correct is:
- Increase heart rate
Typical for Lipid soluble drugs is:
— Small distribution volume
— Big distribution volume
— Volume distrib doesn’t depend on lipid solubility
Correct is:
— Big distribution volume
Explain therapeutic Index:
Therapeutic index (TI): a measurement of the safety of a drug
TI = median toxic dose (TD50)/median effective dose (ED50)
The greater the therapeutic index, the safer the drug
High therapeutic index: e.g., glucocorticoids, penicillin
TI is the difference between max dose possible giving therapeutic effect in 50 % of cases and the min dose giving 50% of pats toxic effect.
Difference bn PK and PD:
PD focuses on effect on body excerted by the drug. gives knowledge on body in Effect vs conc graph.
PK focuses on effect of doses in absorption rate, elimination. Giving knowledge on the drug. in a conc vs time graph.
PK interaction example: Opioid delays its own absorption by decr intestinal motility. So effect is delayed.
PD interaction example: Calcium or iron worsens absorption of tetracyclin
What is Dantrolene?
Long lasting NMJ blocker
Acidification of urine:
Accelerates excretion of basic/alkali drugs
In Vitro experiment, admin of NITROPRUSSIDE to a bath produce:
- Relaxation of concentrated arterial ring(after prev adm of NorAdr)
.
Acetylcholine contracts ileum by which Receptor?
- Nicotinic
- Muscarinic
- Alpha-1 Treat
- Muscarinic (bc in NMJ gives effect of contr)
Nicotine addiction
VareNICLINE
Benzodiazepine MoA, Use, example:
- Use: Anti-anxiousness, Hypnotic, Sedative, Anti convulsive, treat sleep insomnia, panic attack.
- MoA: Indirect GABAA receptor agonism → ↓ neuronal excitability
(Enhance effect of neurotransmitter GABA by binding on the GABA Receptors alpha- subunit
- Binding site of Chlorine-Channel..→Cl influx –> Hyperpolarization→cannot conduct AP →CNS depression)
- Ex: Diazepam(Valium)
Carbon anhydrase inhibitor, MoA, AE, Use:
- Moa: inhibit carbon anhydrase which normally reduce formation of Hydrogen and Bicarb from CO2 and Water in Prox tubule Kidney.
- Inhibition of this leads to Excretion of Na, Bicarbonate, K and Water, in urine.
- Use: anti glaucoma, treat HT, diuretic, Anti-epileptic.
- AE: Metabolic acidosis. Because loss of bicarbonate in urine. Alkalic urine(high bicarbonate)
increase risk of Kidney Stones.
Administration of norepinephrine to an experimental animal induces:
- severe tachycardia and increased blood pressure
- increased blood pressure
- increased in systolic and diastolic blood pressure
- decreased blood pressure if taken with alfa1-blockers
Correct is:
- decreased blood pressure if taken with alfa1-blockers
Atropine prevents the effect of neostigmine on:
- neuromuscular junction
- muscarinic receptors
- nicotinic receptors in ganglia
Correct is:
muscarinic receptors
Isoprenaline stimulates:
- β1 and β2 receptors
- β2 receptors
- M receptors
Correct is:
- β1 and β2 receptors
Tyramine:
- is a direct acting sympathomimetics
- can be dangerous in a combination with MAO inhibitors
- is usually well absorbed from GIT
Correct is :
— can be dangerous in a combination with MAO inhibitors
Opioid dependence treatment drugs:
Acute intoxication: Naloxone
1 st line drugs is for long term substitution and to decrease abstinence: methadone
Decrease craving: Tiapridal
Decrease drug-induced euphoria: Naltrexone
Neostigmine effect on the eye:
Inh AchE=> miosis (small pupils)
Explain volume distribution:
- Give extent of drug penetration in body, aka extent of drug moving from central to
peripheral component of body
— The theoretical volume a drug would occupy if it was distributed evenly in fluids at plasma concentration.
— Provides information about a drug tendency to distribute in other compartments (e.g., muscle or adipose tissue) rather than in the plasma.
— Drugs can distribute in more than one compartment.
— The Vd of plasma protein-bound drugs may be increased in patients with renal and liver disease due to loss of plasma proteins.
Vd = M/Cplasma
Explain saturation kinetics:
Saturation kinetics:
Such substances can have first-order kinetics at lower plasma concentrations and after saturation of the processes involved in their elimination (most often liver enzymes), they are eliminated at a constant rate - i.e. by zero-order kinetics.
Few substances are used in pharmacotherapy whose therapeutic plasma concentrations are high enough to saturate the enzymes. Typical examples are salicylates, ethanol and phenytoin.
Michelis-mentens kinetics
- When the enzymes responsible for met of drug are saturated by the drug, no matter the
increased dose, the rate of metabolism cannot go faster.
- Small increase of dose gives big increase in plasma cons. – careful for toxicity.
1st order kinetics
- T0,5 is constant (zero order has t1⁄2 increasing w dose, but is itself independent of dose remaining in plasma)
First order kinetics: The rate of metabolism and/or elimination is directly proportional to the plasma concentration of the drug (Cp decreases exponentially over time)
First-order is a flow-dependent elimination.
Applies to most drugs
Zero order kinetics
Zero order kinetics: The rate of metabolism and/or elimination remains constant and is independent of the plasma concentration of a drug at steady state (Cp decreases linearly over time)
Zero-order is a capacity-limited elimination.
Examples include ethanol, phenytoin, aspirin (at high concentrations)
Explain withdrawal syndrome
- Related to long administration and sudden stop
- Is the symptoms occurring upon sudden end of long term use of a drug.
- The symptoms are usually the opposite of the effect of the drug, due to the body developed
physiological dependence to the drug, by negative feedback. - In addictive drugs, even so called Abstinence occur, with negative mood swings and cravings
etc.
Presents with:
Agitation, Anxiety, Tremor, Insomnia, Sweating, Salivation, Diarrhea, Collapses,
- SOLUTION: Tapered→Gradual drug withdrawal
- Ex: Corticosteroid stop → Adrenal insufficiency
- Ex: Benzodiazepines (anti Panic Attack drug)→Panic attack, sleep disturbance, irritability
(because it is addictive too), anxiety/tension. - Ex: Anti Epileptic (Phenytoin)→epileptic seizure
Adverse drug reaction type F
Unexpected failure of therapy.
Dose Dependent. Common. Usually due to drug interactions.
Solved by increasing the dose.
Ex: contraceptives fail when taken with specific enzyme inducers(alcohol)
Main elimination organs of drugs:
liver, kidney
Tubocurarine Induces HypOtension how?
- by blocking ganglion and through the release of Histamine
What is drug interaction?
When a substance/drug enhance or decrease the PD(effect wo changing drug) or the PK(abs, elim, metab by changing drug) of another drug.
- Agonism: promote
- Antagonism: no effect
• additive effect (1+1=2)
• synergistic (hyperadditive) effect (1+1>2) • potentiation (1+0>1)
• combination therapy:
increased therapeutical effect
dose can be decreased decreased toxicity (antihypertensives, analgesics, antidiabetics)
Name the clinical uses of adrenaline:
Cardiac arrest - resuscitation, Anaphylactic shock, hypotension associated with septic shock, Asthma, spf. Bleeding (nosebleeds)
Effect of noradrenaline on the heart rate:
Through beta 1 and alpha 1 effect increases heart rate, CO and BP→baroreceptor reflex→ decreased heart rate
Isoprenaline is a:
Pure beta agonist
Administration of Adrenaline to animal induce:
- Increased BP
- Severe tachycardia and possible increase of BP
- Increase systolic and possible Diastolic BP
- Decrease BP when admin with Alpha-1-blocker Prasozin.
- Decrease BP when admin with Alpha-1-blocker Prasozin.
Adrenaline caused an increase in systolic blood pressure, a decrease in diastolic blood pressure, and an increase in heart rate.
Adm of NorAdr to animal induce:
- Tachycardia and light increase of BP
- Increase BP and less significant increase of HR
- Increase of Systolic and Decrease of Diastolic BP
- Decr BP when admin with alpha-1-Blocker Prasozin
Decr BP when admin with alpha-1-Blocker Prasozin
Severe benzodiazepine overdose can be reversed with:
— Naloxone
— Disulfiram
— Flumazenil
Flumazenil
Alkalization of urine:
a) accelerates the excretion of acidic drug
b) accelerates the excretion of basic drug
c) accelerates the excretion of all drugs
- Alkalization of urine:
a) accelerates the excretion of acidic drug
Example of psychomimetic (hallucinogenic):
LSD, Marijuana, Amphetamines, Ecstasy=MDMA, ketamine,
Drugs for the treatment of neuropathic pain (first line therapy)
Tricyclic Antidepressants, Serotonin Reuptake Inhibitor, Antiepileptics, Lidocaine plaster
Potentiation means:
— one drug increases the effect of another drug without having the same effect
— two drugs have additive effect when administered together
— one drug blocks the effect of another drug
— two drugs have additive effect when administered together
Atropine will oppose the effect of:
— Morphine on the intestinal smooth muscle
— Acetylcholine on the intestinal smooth muscle
— Histamine on the Intestinal smooth muscle
— Acetylcholine on the intestinal smooth muscle
Atropine is a competitive antagonist of the actions of acetylcholine and other muscarinic agonists.
The effect of the drug absorption (exposure) is best characterized by
—The Volume of Distribution
— The area under the concentration time curve (AUC)
The area under the concentration time curve (AUC)
Some drugs are effective in the treatment of neuropathic pain when administered locally:
—Dobutamine
—Carbamazepine
— Capsaicin
Capsaicin
Which of the following drugs are NOT commonly used in psoriasis?
— Emollients
— topical antivirals
— Vitamin D Analogs
Topical antivirals
