Drugs Involved in Dyslipidemia and Obesity Treatment: Focus on Adipose Tissue

Table 2

Drugs used in obesity: classical effects, effects on adipose tissue, and weight.

Drugs used in obesity	Classical mechanism of action	Adipose tissue effects									Appetite regulation
		AT mass/AT depots	Glucose metabolism/insulin sensitivity	Lipid metabolism	Adipocytokine expression		Antiatherogenic	Adipogenesis	Browning effect	Anti-inflammatory
					↑	↓
Orlistat	Reversible inhibitor of gastric and pancreatic lipase		⊕ [159, 160]	⊕ lipolysis [160]		Leptin [160]
Sibutramine	Sympathomimetic amine; inhibition of NA and 5-HT reuptake			↓ TG [164]; ↑ HDL [164]	Adiponectin [164]	Leptin and resistin [164]	↓ CRP [164]
Diethylpropion	Sympathomimetic amine; inhibition of NA, 5-HT; DA reuptake										⊝ [165]
Phentermine	Sympathomimetic amine; noradrenergic modulation; DA receptor agonist										⊝ and promotes saciety [166]
Lorcaserin	5-HT2c receptor agonist										⊝ and promotes saciety [167, 168]
Naltrexone and bupropion	Antagonist of opioid receptors in POMC neurons and inhibitor of reuptake of NA and DA	↓, mainly VAT [170]
Topiramate	Antagonist of AMPA receptors and stimulation of GABA receptors		⊕ [171]		Adiponectin [171]	Leptin [172]			⊕ UCP 2/3 expression [172]		⊝ [172]
Liraglutide	GLP-1R agonist	↓ [175, 182–188]; mainly VAT [175–178, 182–187]	⊕ [178, 182, 185, 192]	⊕ FA oxidation [182, 188]; ⊝ lipogenesis [176]	Adiponectin (in dysfunctional adipocyte) [189, 197]; omentin [192]	TNFα [181]	↓ CRP and sICAM-1 levels [175]	⊕ [194]	⊕ [180, 182, 188]	Vide adipokine regulation	⊝ and promotes saciety and improves eating behaviour [175–180]

⊕: stimulates; ⊝: inhibits; AT: adipose tissue; TG: triglycerides; HDLs: high-density lipoproteins; CRP: C-reactive protein; NA: noradrenaline; 5-HT: 5-hydroxytryptamine; DA: dopamine; POMC neurons: pro-opiomelanocortin neurons; VAT: visceral AT; AMPA receptors: a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors; GABA receptors: γ-aminobutyric acid receptors; FA: fatty acid; TNFα: tumour necrosis factor α; GLP-1R: glucagon-like peptide 1 receptor; sICAM-1: soluble intracellular adhesion molecule-1.