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“Designer drugs” (referred as synthetic drugs, research drugs/chemicals) are synthesized by drug dealers and chemists illicitly to elicit euphoric and psychostimulatory actions.  These drugs are structural congeners of illegal and/or banned abusive substances and exhibit pharmacological effects similar to their parent drug.  Moreover, due to its designed structural difference to circumvent drug laws, these can be currently obtained legitimately and readily in common stores and through internet.  Alarmingly, several designer drugs are significantly toxic and perilous as compared to their corresponding street drug. Piperazine derivatives have been designed by substituting various chemical groups to the basic piperazine moiety to have a stimulatory effect. Various drugs with piperazine structural moieties are Benzylpiperazine-(BZP), 2C-B-BZP, CDPP, DBZP, MBZP, mCPP, MCDZP, MeOPP, pCPP, pFPP, and Trifluoromethylphenylpiperazine-(TFMPP). The most commonly abused piperazine derivatives are BZP, TFMPP and mCPP.  But, there are few articles that have revealed the prevalence and toxic actions of TFMPP.  Hence, in this review, we focus on pharmacodynamic, pharmacokinetic and toxic effects of TFMPP.  Similar to other stimulants, TFMPP also increases the monoaminergic neurotransmission. Interestingly, TFMPP principally affects the serotonergic neurotransmission. TFMPP displays significant agonistic activity towards 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_2C receptors, except the 5-HT_2A receptor, where it acts as a weak partial agonist or antagonist. On the other hand, TFMPP has insignificant affinity towards 5-HT₃ receptor. It also affects release of acetylcholine and the release and uptake of monoaminergic neurotransmitters (dopamine, norepinephrine). Due to the specific effects of TFMPP on serotonergic neurotransmission, it induces hallucination, psychotropic effect, anxiety, nociceptic effect, hypothermia, hypotension, and bradycardia. Furthermore, it has a great impact on various behavioral activities such as aggression, avoidance, anxiety, sexual activities, feeding and accommodation. Conversely, if suitable prophylactic and therapeutic measures are not considered immediately, TFMPP can be an impending danger for the global health care.