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Pharmacology MBBS > General Pharmacology part 1 > Flashcards

General Pharmacology part 1 Flashcards

1
Q

Father of pharmacology

A

Oswald Schmiedeberg

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2
Q

Define drug

A

Any substance or product that is used or intended to be used to modify or explore physiological and pathological states for the benefits of the recipient

Two types: pharmacodynamic and chemotherapeutic

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3
Q

Clinical pharmacology

A

It includes pharmacodynamic and pharmacokinetic investigation in healthy volunteers as well as patients

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4
Q

The molecular weight of most drugs is in the range of ___ and why

A

100 D -1000 D
Large enough to have specific characteristics
Small enough to pass through membranes

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5
Q

Sources of drugs

A
  1. Plants (alkaloids, glycosides, oils,…)
  2. Animals
  3. Microbes (antibiotics)
  4. Minerals
  5. Synthetic (rational drug designing)
  6. Biotechnology
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6
Q

Drugs derived from animal sources

A

Exenatide

Lepirudin (anticoagulant)

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7
Q

Semisynthetic drugs examples

A

Apomorphine

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8
Q

Modified insulin

A 
Examples
Glulisine, lispro, aspart 
Made by changing the sequence of gene
Change in onset and duration of action
There are structural changes
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9
Q

What are BAN ,USAN and rINN

A

These are the naming guidelines for non proprietary names of drugs
For older drugs it was named according to
British Approved Name
US Adopted Name,…

But for newer drugs it is according to recommended International Nonproprietary Name

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10
Q

The first drug discovered to act on the ANS

A

Reserpine

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11
Q

What are the pros and cons of drugs marketed under brand / proprietary names

A

Pros
To ensure consistency of product for quality and bioavailability and are not generic like those prescribed on the basis of the generic name

Cons

  1. More expensive for marketing
  2. Less uniformity and convenience
  3. Less better in comprehension as brand names have no relation to each other
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12
Q

Pharmacopoeias and formularies, the types of drug compendias (drug compilations)

A

Pharmacopoeias contains the description of chemical and physical characteristics of drugs hence useful for drug manufacturers and regulatory authorities
Eg., Indian Pharmacopeia IP

Formularies are easily carried booklets which contains biological properties of drugs useful for doctors
Eg., National Formulary of India NFI

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13
Q

Examples of major unofficial compendiums

A
  1. Martindale: The complete drug reference (extrapharmacopoeia) by Britain
    From USA:
  2. Physicians desk reference (PDR)
  3. Drug facts and compilations
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14
Q

Essential drugs

A

Those which satisfy the priority healthcare needs of the nation that are economical and safe
They should be preferably single compounds

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15
Q

Orphan drugs

A

Drugs which are not economical and affects less number of people (0.2 million according to USA)
Government incentives are given

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16
Q

Major types of medical powders

A

Bulk powder: powder for topical application are supplied as bulk powder in metabolic and plastic containers with holes for sprinkling

Effervescent powder contain granulated sod, bicarbonate and citric or tartaric acid. The react when dissolved in water to produce bubbling

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17
Q

Different types of tablets

A
  1. Chewable tablets
  2. Dispersable tablets
  3. Sublingual tablets
  4. Enteric coated tablets
  5. Sustained / Extended release tablets
  6. Controlled release tablets
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18
Q

Different types of capsules

A
  1. Soft gelatin capsules: dissolves rapidly, generally contains a liquid medicament
  2. Enteric coated capsules
  3. Spansules: extended release capsules which are packed with granules of the drug having different coatings to dissolve over a period of time
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19
Q

Lozenges

A

Tablet like bodies containing the drug along with a suitable gum , sweetening and flavouring agents
They are retained in the mouth and allowed to dissolve very slowly, providing local action for mouth and throat

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20
Q

Suppositories and its derivatives

A

Suppository is a clinical bullet shaped dosage form for insertion in the anal canal, in which the drug is mixed with a mouldable form base that melts at high temperature and releases the stored drug

Pessaries: are oval or suitably shaped bodies for vaginal insertion
Bougies: elongated pencil like cones for insertion into male or female urethra

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21
Q

Syrups and their derivatives

A

Syrups: Sweet hydro alcoholic derivatives of drugs

Elixirs: less sweet and thick compared to syrups

Dry syrups: for drugs that are unstable in water
They must be reconstituted with water

Linctus: viscous syrupy liquid meant to be licked slowly for soothing the throat

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22
Q

Lotions and their derivatives

A

Meant for external applications without rubbing
They usually have soothing, cooling, protective or emollient property

Liniments are similar preparations which are usually contain counterirritants and are to be rubbed on the skin to relieve pain and cause rubefaction

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23
Q

Injections are supplied through

A

Ampoules and vials

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24
Q

Ointments and creams

A

In ointments, drugs are incorporated in an oily base (wax,…). They are not suitable for oozing surfaces.
Good for dry chronic lessons

In creams, the base is a water in oil emulsion. The drug is better absorbed and are cosmetically more acceptable

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25
What are PMDIs
Pressurised metered dose inhaler are hand held devices which use a propellant (hydro fluoro alkane) and deliver the specified drug in aerosol form in actuation
26
Jet nebulisers
Jet nebulisers produce a mist of drug solution generated by pressurised air or oxygen
27
Rotahaler
Rotahaler is device in which a portable capsule (rotacap) containing very fine powder of drug is punctured during actuation and the released particles are aerosolised by the inspiratory airflow
28
Particle size of aerosolised drug
1-5 micrometer for effective deposition in the bronchioles Larger in the oropharynx Smaller do not settle and are exhaled out
29
Dosage forms of drugs
1. Solid forms (powder, tablets, pills, capsules, lozenges and suppositories) 2. Liquid forms (aqueous, suspensions, elixirs, drops, lotions, injections) 3. Semisolid forms (ointments, pastes, gels) 4. Inhalations
30
Limitations of oral route of administration
1. Slower action 2. Unpalatable drugs cannot be used 3. May cause nausea and vomiting 4. Cannot be used for unconscious, uncooperative or vomiting patient 5. Absorption of drug may be variable or erratic (streptomycin) 6. Maybe destroyed by liver (first pass metabolism) or by digestive juices
31
Buccal or sublingual route of administration of drugs
Only lipid soluble and non irritant drugs can be used Can be spat after the effect has been obtained Relatively rapid Liver is bypassed Examples: GTN, buprenorphine, desamino-oxytocin
32
Drugs which are sometimes given rectally
Diazepam, paracetamol, indomethacin, ergotamine | 50% bypass liver
33
Advantages of TTS
Transdermal therapeutic patches 1. Smooth plasma concentrations 2. Decreased inter individual variations, due to little first pass metabolism 3. Decreased side effects But they are costly
34
Drugs absorbed via nasal route
GnRH agonists, calcitonin, desmopressin
35
Dermojet
High velocity jet of drug solution is protected from a micro fine orifice using a gun like implement A type of subcutaneous parental route Generally painless and suited for mass inoculations
36
Pellet implantation
Drugs in the form of solid pellet is introduced with a trochar and cannula Sustained release over weeks or months Examples: DOCA, testosterone
37
Sialistic (non biodegradable) and biodegradable implants
Crystalline drug is packed in tubes or capsules made of suitable materials and implanted under the skin Slow and uniform leaving of drug occurs over months Examples: hormones and contraceptives (Norplant)
38
Intramuscular route
Drug is injected into a large muscle (less innervation but more vascular) like ...,triceps, rectus femoris,... Self injection is often impractical because deep penetration is required Oily or aqueous solutions can be used Avoided with anticoagulant treated patient since it may cause local haematoma
39
Intravenous | Advantages and risks
1. Highly irritant drugs can be used (insensitive intima and dilution) 2. Rapid. Dose is smallest as bioavailability is 100% 3. Large volumes can be infused 4. Titration with dose can be possible Risks are: 1. Thrombophlebitis of the injected vein 2. Necrosis of adjoining tissues of extravasation occurs
40
IV disadvantages
1. Only aqueous solutions can be used 2. Risk of air embolism 3. Most risky route
41
Intradermal injection
The drug is injected into the skin causing a bleb (BCG vaccine, sensitivity testing) or scarring/multiple puncture of epidermis through a drop of drug is done For specific purposes only
42
Routes of drug administration
A) Local routes: topical, deeper, arterial B) Systemic routes: oral, buccal, rectal, cutaneous, inhalation, nasal, parenteral ; 1. Subcutaneous (dermojet, pellet implantation, implants) 2. Intramuscular i.m. 3. Intravenous 4. Intradermal injection
43
Filtration is the mechanism of absorption of which type of drugs
Water soluble drugs through aqueous channels
44
Antimicrobials requiring dosage reduction even in MILD renal failure
``` Acyclovir Aminoglycosides Amphocetericin B Cephalexin Ethambutol Vancomycin ```
45
Relationship between pH and absorption and excretion of drugs Ion trapping
Generally acidic drugs (aspirin,...) are absorbed from stomach and vice versa Within the gastric cell, the drug is ionised (pH=7) and then passes only slowly to the extra-cellular fluid (ion trapping) This may contribute to gastric mucosal cell damage caused by aspirin Acidic drugs are excreted more in alkaline urine and vice versa Basic drugs attain higher concentration intercellularly
46
Drugs which are actively transported
Levodopa and methyl dopa are actively transported by aromatic amino acid transporter P-glycoprotein to deal with zenobiotics
47
Significance of redistribution of drugs
Highly lipid soluble drugs undergo more redistribution They are very short acting (less time in systemic circulation) Eg., thiopentone
48
Drug action types
1. Stimulant 2. Depressant 3. Irritant 4. Replacement 5. Cytotoxic
49
Mechanism of drug action
1. Physical 2. Chemical 3. Enzymes 4. Ion channel 5. Transporter 6. Receptor
50
Antimicrobials which need dosage reduction only in severe renal failure
``` Carbenicillin Cefotaxime Ciprofloxacin Cotrimaxazole Metronidazole Norfloxacin ```
51
Drugs having cumulative effect (accumulated in the body)
1. Full loading dose of digoxin should not be given to the patient if he has received it within the past week 2. A course of emetine should not be repeated within 6 weeks
52
Placebo reactors | Examples of placebos
People who will easily respond to placebo Examples: lactose tablets/ capsules, distilled water injection, multi vitamin preparations (Nocebo is the negative psychodynamic effect)
53
Factors affecting absorption of drug
1. Aqueous solubility 2. Concentration 3. Area of absorbing surface 4. Vascularity 5. Route of administration 6. Bioavailability
54
Does faster gastric emptying accelerate drug absorption? Why
``` Yes The absorption of almost all drugs is low (even for acidic drugs) in stomach because of: 1. Thick mucosa 2. Covered with mucus 3. Low surface area ```
55
Drugs and food
Food dilutes the drug and generally reduces absorption Certain drugs form poorly absorbed complexes (tetracycline with Ca of milk) One exception is the absorption of lumefantrine with fatty food
56
P-gp
The oral absorption of certain drugs is reduced by the efflux transporter (actively) P-gp of intestinal lumen Free systemic elimination (part of first pass metabolism) May be developed by tumour cells Examples: digoxin , cyclosporine which are metabolised by CYPA4
57
Inhibitors of P-gp
Verapamil (used to reverse anti cancer resistance ) Amiodarone Cyclosporine Itraconazole Nifedipine Erythromycin and Quinidine These inhibitors increases the oral bioavailability of certain drugs
58
P-gp inducers
Phenobarbitone Rifampin The reduce the oral bioavailability of certain drugs
59
Luminal effect of drugs
Formation of insoluble complexes due to the interaction between drugs which decreases absorption Examples: 1. tetracyclines and iron preparations with calcium salts and antacids 2. Phenytoin with sucralfate This can be minimised by administering the drugs at 2-3 hour intervals
60
Examples of urine acidifiers for removing toxicity of alkaline drugs
Ammonium chloride Vitamin C Cranberry juice (Bicarbonate for alkalinisation)
61
Henderson Hasselbach’s equation
For an acidic drug: Log(u/i) = pKa - pH For basic unionised and ionised trade places pKa is the pH of the medium at which 50% of drugs is ionised and 50% is unionised.
62
Drugs which affect gut wall motility
Anticholinergics, tricyclic depressants and opioids retard motility while metoclopramide increases it
63
Drugs which cause mucosal damage
Neomycin Methotrexate Vinblastine
64
Drugs which penetrate intact skin
``` Hyoscine Fentanyl GTN Nicotine Testosterone Estradiol ```
65
Cornea as a drug route
It is permeable to lipid soluble unionised physostigmine but not to highly ionised neostigmine Timolol eye drops get absorbed through nasolacrimal duct to produce bradycardia and asthma
66
Bioavailability (f)
It is the fraction of unchanged drug which reaches the systemic circulation It depends on absorption and first- pass metabolism
67
Calculation of bioavailability
Bioavailability = AUC_oral/ AUC_iv * 100 | Area under the curve which is trapezoid for oral and hyperbolic for IV
68
Cross tolerance
Development of tolerance to pharmacologically related drugs Closer, the more complete the cross tolerance Examples: Alcoholics are tolerant to barbiturates and general anaesthetics
69
Mechanisms of tolerance of drugs
1. Pharmacokinetic/ drug disposition tolerance: The effective concentration of the drug is decreased, mostly due to enhancement of drug elimination on chronic use Barbiturates and carbamazepine induce their own metabolism Amphetamine accelerate its own renal elimination 2. Pharmacodynamic/ cellular tolerance: Cells become less responsive
70
Tachyphylaxis
Rapid development of tolerance when doses of drug repeated in rapid succession. Usually seen in indirectly acting drugs like ephedrine, tyramine, nicotine,... These drugs act by releasing the catecholamines of the body which can get depleted soon. This is one mechanism
71
Corticosteroids should be taken at what time of the day and why
Single morning dose | Due to more pituitary-adrenal suppression at night
72
Statins are more effective at what time of the day
Late evening HMG CoA is reductase is more active in the evening But statins have longer half lives when taken at the day time But atorvostatin and rosuvastatin have half lives of 20-30 hours so it can be taken at any part of the day
73
For which type of drugs are loading dose required
For drugs with long t1/2 Since several days would be wasted to acquire the required therapeutic effect, an initial loading dose is given followed by maintenance doses Example: chloroquine
74
How does probenecid increase the duration of action of penicillin
Probenecid is an organic acid which has high affinity for tubular OATP (organic anion transporting polypeptides) It blocks active transport of penicillin and decreases tubular secretion of penicillin
75
Examples of hit and run drugs
Organophosphate and anticholinesterases Reserpine drugs with irreversible action Clopidogrel
76
Bioequivalence of drugs
Two pharmaceuticals equivalent compounds that are similar in rate and extent of absorption
77
FDA criteria for approval of generic drug
Bioequivalence = +- 20% of the existing (branded) drug
78
Pharmacognosy
The study of extraction, purification and analysis of drugs obtained from plants.
79
Ethnopharmacology
The interdisciplinary scientific exploration of biologically active agents traditionally employed or observed by man

Pharmacology MBBS (19 decks)

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