Synthetic non-steroidal hormone

Synthetic steroid hormone. ***Synthetic steroid hormone*** - **Tibolone** is a **synthetic steroid** with **estrogenic, progestogenic, and weak androgenic properties** used for hormone therapy in postmenopausal women. - Its structure is derived from **nortestosterone**, making it a synthetic compound rather than naturally occurring. *Natural steroidal hormone* - Natural steroidal hormones like **estrogen** and **progesterone** are produced endogenously by the body and have specific steroidal molecular structures. - Tibolone is not a naturally occurring hormone but is manufactured in a lab. *Natural non-steroidal hormone* - Natural non-steroidal hormones typically include peptides (e.g., insulin) or amines (e.g., thyroid hormones). - Tibolone's chemical structure is clearly steroidal, not non-steroidal. *Synthetic non-steroidal hormone* - Synthetic non-steroidal hormones are compounds like **diethylstilbestrol** (DES) that mimic hormone action but lack the steroid nucleus. - Tibolone possesses a distinct steroid backbone, classifying it as a synthetic steroid.

NEET-PG 2012 — Pharmacology

Q: Which of the following is used in the second-line management of strychnine poisoning?

Barbiturates. ***Barbiturates*** - As a **second-line treatment**, barbiturates like phenobarbital are used to control **refractory seizures** and muscle spasms in strychnine poisoning when benzodiazepines are insufficient. - They enhance the effect of **GABA**, leading to central nervous system depression and muscle relaxation. *Physostigmine* - This is an **acetylcholinesterase inhibitor** and is primarily used to reverse the anticholinergic effects of certain poisonings, not strychnine. - It would worsen seizures by increasing **acetylcholine**, which can cause tremors and convulsions. *Naloxone* - Naloxone is an **opioid antagonist** used to reverse opioid overdose, which presents with respiratory depression and pinpoint pupils. - It has no role in treating strychnine poisoning, which primarily causes **muscle spasms** and seizures. *Diazepam* - Diazepam, a **benzodiazepine**, is the **first-line treatment** for seizures and muscle spasms in strychnine poisoning. - It works by enhancing the effects of **GABA** at the GABA-A receptor, thereby reducing neuronal excitability.

Q: Oximes are contraindicated in which poisoning:

Carbamate. ***Carbamate*** - Traditionally, oximes were considered **contraindicated** in carbamate poisoning based on concerns they could worsen the **cholinergic crisis** by reactivating carbamylated acetylcholinesterase. - Carbamates spontaneously **decarbamylate** from acetylcholinesterase within minutes to hours, so their inhibition is typically **short-lived and reversible**. - **Clinical relevance**: While modern evidence suggests oximes are more likely **ineffective** rather than harmful in carbamate poisoning, they are generally **not recommended** as they provide no therapeutic benefit. For exam purposes, particularly in historical contexts (NEET 2012-2013), carbamate poisoning is the answer for oxime contraindication. *Diazinon* - Diazinon is an **organophosphate**, and oximes like pralidoxime are **strongly indicated** for reactivating **acetylcholinesterase** inhibited by organophosphates. - Oximes are a crucial part of recommended antidotal therapy alongside **atropine** for severe organophosphate poisoning. - Must be administered early (within 24-48 hours) before **aging** of the phosphorylated enzyme occurs. *Phorate* - Phorate is a highly toxic **organophosphate pesticide**, and oximes are **indicated** for treatment of phorate poisoning. - Oximes work by **dephosphorylating** (nucleophilic attack on) the acetylcholinesterase enzyme, which has been inhibited by the organophosphate, restoring its catalytic function. *Malathion* - Malathion is an **organophosphate insecticide**, and oxime reactivators are **effective** in malathion poisoning. - The mechanism involves **cleaving the phosphate bond** from the serine residue on the acetylcholinesterase enzyme, allowing it to metabolize acetylcholine again and reverse cholinergic toxicity.

93 Questions — Page 10 of 10

Q91

Tibolone is a ?

Q92

Which of the following is used in the second-line management of strychnine poisoning?

Q93

Oximes are contraindicated in which poisoning: