Spotting held in MD Pharmacology Exam

1. Spotting in MD
Pharmacology
Exam
Presenter:
Dr Arun Singh
Senior Resident
Department of Pharmacology
SMS Medical College, Jaipur

2. Claviceps purpurea
• The ergot sclerotium contains high concentrations (up to 2% of
dry mass) of the alkaloid ergotamine, a complex molecule
consisting of a tripeptide-derived cyclol-lactam ring connected
via amide linkage to a lysergic acid (ergoline) moiety, and
other alkaloids of the ergoline group that are biosynthesized by
the fungus.
• Ergot alkaloids have a wide range of biological
activities including effects on circulation and
neurotransmission.
• Ergotism is the name for sometimes severe pathological
syndromes affecting humans or animals that have ingested
ergot alkaloid-containing plant material, such as ergot-
contaminated grains. Monks of the order of St. Anthony the
Great specialized in treating ergotism victims.

3. • The neurotropic activities of the ergot alkaloids may also
cause hallucinations and attendant irrational behaviour, convulsions,
and even death.
• Other symptoms include strong uterine contractions, nausea, seizures,
and unconsciousness. Since the Middle Ages, controlled doses of ergot
were used to induce abortions and to stop maternal bleeding after
childbirth.
• Ergot alkaloids are also used in products such
as Cafergot (containing caffeine and ergotamine or ergoline) to treat
migraine headaches. Ergot extract is no longer used as
a pharmaceutical preparation.
• Ergot contains no lysergic acid diethylamide (LSD) but rather
ergotamine, which is used to synthesize lysergic acid, an analogue of
and precursor for synthesis of LSD. Moreover, ergot sclerotia naturally
contain some amounts of lysergic acid.

4. Poppy Flower
• Papaver rhoeas, with common
names including common poppy, corn
poppy, corn rose, field poppy, Flanders poppy,
and red poppy, is an annual herbaceous species of
flowering plant in the poppy family Papaveraceae.
• It is notable as an agricultural weed (hence the
common names including "corn" and "field").
• Especially in the Commonwealth, it is used a
symbol of remembrance of the fallen soldiers and
other military, during World War I and thereafter.

5. • Before the advent of herbicides, Papaver rhoeas was often abundant in
agricultural fields, as the plant thrives in areas of disturbed soil.
• Flushes of poppies may still appear in fields where herbicides are not
used, as well as those in fallow.
• The corn poppy and its cultivars such as the Shirley poppy are widely
grown in gardens and are frequently found in packets of seed labelled
"wildflower mixes“.

6. Foxglove Flowers
• Foxglove, (genus Digitalis), genus of about 20
species of herbaceous plants (family
Plantaginaceae).
• Foxgloves are native to Europe, the Mediterranean
region, and the Canary Islands, and several species
are cultivated for their attractive flower spikes. All
parts of the plants contain poisonous
cardiac glycosides and are considered toxic if
ingested.

7. Physical description--
• Foxgloves typically grow to a height of 45 to 150 cm (18 to 60 inches).
They produce alternating, ovate to oblong leaves toward the lower part
of the stem, which is capped by a tall one-sided cluster of somewhat
pendulous bell-shaped flowers, each of which may be up to 6.5 cm (2.5
inches) long. The flowers may be purple, yellow, or white and are often
marked with spots within. Most species are biennials, meaning that they
flower during their second year and then die after seeding. The fruits are
dry capsules with numerous small seeds.
Use--
• The common, or purple, foxglove (Digitalis purpurea) is a popular
garden ornamental, and numerous hybrids and cultivars have been
developed in a range of colors.

8. Atropa Belladonna
• Atropa belladonna, commonly known
as belladonna or deadly nightshade, is a
toxic perennial herbaceous plant in the nightshade
family Solanaceae,which also
includes tomatoes, potatoes,
and eggplant (aubergine).
• The foliage and berries are extremely toxic when
ingested, containing tropane alkaloids.
• These toxins include atropine, scopolamine,
and hyoscyamine, which
cause delirium and hallucinations, and are also used
as pharmaceutical anticholinergics.

9. • Tropane alkaloids are of common occurrence not only in the Old-
World tribes Hyoscyameae (to which the genus Atropa belongs)
and Mandragoreae, but also in the New World tribe Datureae - all of
which belong to the subfamily Solanoideae of the plant family
Solanaceae.
• Atropa belladonna has unpredictable effects. The antidote for
belladonna poisoning is physostigmine or pilocarpine, the same as
for atropine.

10. Fixed Dose Combinations of Sacubitril /
Valsartan
• Sacubitril is an orally active neprilysin inhibitor
which prevents the degradation of endogenous
ANP, BNP and other vasodilator peptides,
producing vasodilatation, natriuresis and diuresis.
• Combined with the ARB valsartan, it has been
recently approved for use in advanced heart failure
to decrease the incidence of death and acute
decompensation.
• A greater reduction in hospitalization and mortality
compared to enalapril has been reported.

11. • Neutral endopeptidase (NEP; neprilysin) inhibitors: This is a new class of drugs
which inhibit NEP enzymes that degrade NPs, bradykinin, substance P and
adrenomedullin. By raising levels of natriuretic and vasodilator peptides they have
potential utility in CHF.
• A nonpeptide NEP inhibitor Sacubitril has been approved (in 2015) for the
treatment of class II to IV CHF when combined with the ARB valsartan.
• Sacubitril: It is an orally active NEP inhibitor which increases the blood levels of
NPs and other vasodilator peptides resulting in natriuresis, diuresis, vascular
relaxation, lowering of AngII as well as aldosterone levels.
• Combined with valsartan, it affords symptomatic improvement in CHF patients.
• Sacubitril is a prodrug that is absorbed after oral ingestion and rapidly activated by
esterases to sacubitrilat.

12. • The absolute oral bioavailability is 60%, and food does not alter
absorption.
• Passage of sacubitrilat across blood-brain barrier is limited and it is not
significantly metabolized further.
• Excreted in both urine and faeces, the plasma t½ of sacubitrilat is ~12
hours. No significant drug interactions with drugs generally used in
CHF have been observed.
• In a large multicentric randomized clinical trial (PARADIGM-HF,
2014), a 1:1 combination of sacubitril + valsartan (200 mg BD) was
compared with enalapril (10 mg BD) in 8442 patients of class II to class
IV CHF already receiving CHF therapy with one or more of diuretics,
beta blockers and aldosterone antagonist.

13. • The sacubitril-valsartan combination caused 20% greater reduction in
death or hospitalization for heart failure than enalapril.
• The most common side effects were hypotension, hyperkalemia and
renal impairment.
• Angioedema was infrequent, and its tolerability profile was similar to
enalapril.
• Thus, sacubitril-valsartan appears to be a more effective and well
tolerated alternative to ACE inhibitors for reducing morbidity and
mortality in patients with advanced heart failure. However, it is
expensive.

14. Structure Activity Relationship of Fluoroquinolones

15. Structure
Activity
Relationship of
Catecholamines

16. Anaphylaxis
• Anaphylaxis, often known as anaphylactic
shock, is a serious, potentially fatal allergic
reaction and medical emergency that is rapid in
onset and requires immediate medical attention
regardless of use of emergency medication on site.
• It typically causes more than one of the following:
an itchy rash, throat closing due to swelling which
can obstruct or stop breathing; severe tongue
swelling which can also interfere with or stop
breathing; shortness of breath, vomiting,
lightheadedness, loss of consciousness, low blood
pressure and medical shock.

17. • Common causes include allergies to insect bites and stings, allergies to
foods - including nuts, milk, fish, shellfish, eggs and some fresh fruits
or dried fruits; allergies to sulfites - a class of food preservatives and a
byproduct in some fermented foods like vinegar; allergies to
medications - including some antibiotics and non-steroidal anti-
inflammatory drugs (NSAIDs) like aspirin; allergy to general
anaesthetic (used to make people sleep during surgery); allergy to
contrast agents – dyes used in some medical tests to help certain areas
of your body show up better on scans; allergy to latex – a type of rubber
found in some rubber gloves and condom.
• The primary treatment of anaphylaxis is epinephrine injection into a
muscle, intravenous fluids, then placing the person "in a reclining
position with feet elevated to help restore normal blood flow".

18. Difference
between
Angioedema
and
Anaphylaxis
• Angioedema mediated by either an allergic
(histaminergic) mechanism in response to
exposure to foods, drugs, physical stimuli, or
a non-allergic (non-histaminergic)
mechanism (e.g., hereditary angioedema
[HAE], or angiotensin-converting enzyme
[ACE] inhibitor).
• Angioedema is characterized by edema of
the subcutaneous or submucosal tissues,
which can cause airway compromise if the
tongue or larynx is involved.
• Whereas, Anaphylaxis is a life-threatening
systemic allergic reaction characterized by
acute onset and multiorgan involvement.